Panobinostat: An indole and hydroxamic acid derivative that acts as a HISTONE DEACETYLASE inhibitor. It is used as an antineoplastic agent in combination with BORTEZOMIB and DEXAMETHASONE for the treatment of MULTIPLE MYELOMA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
panobinostat : A hydroxamic acid obtained by formal condensation of the carboxy group of (2E)-3-[4-({[2-(2-methylindol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enoic acid with the amino group of hydroxylamine. A histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 6918837 |
| CHEMBL ID | 483254 |
| CHEBI ID | 85990 |
| CHEBI ID | 93774 |
| SCHEMBL ID | 183197 |
| SCHEMBL ID | 164801 |
| SCHEMBL ID | 22773814 |
| MeSH ID | M0540392 |
| Synonym |
|---|
| HY-10224 |
| panobinostat (lbh589) |
| faridak |
| lbh-589 |
| nvp-lbh-589 |
| panobinostat |
| lbh-589b |
| farydak |
| nvp-lbh589 |
| 2-propenamide, n-hydroxy-3-(4-(((2-(2-methyl-1h-indol-3-yl)ethyl)amino) methyl)phenyl)-, (2e)- |
| lbh 589 |
| lbh589 , |
| bdbm29589 |
| AKOS005146046 |
| EC-000.2287 |
| CHEMBL483254 |
| chebi:85990 , |
| BRD-K02130563-001-07-2 |
| panobinostat;(e)-n-hydroxy-3-(4-((2-(2-methyl-1h-indol-3-yl)ethylamino)methyl)phenyl)acrylamide |
| A25218 |
| (e)-n-hydroxy-3-[4-[[2-(2-methyl-1h-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide |
| 404950-80-7 |
| EX-8456 |
| panobinostat [usan:inn] |
| 2-propenamide, n-hydroxy-3-(4-(((2-(2-methyl-1h-indol-3-yl)ethyl)amino)methyl)phenyl)-, (2e)- |
| 9647fm7y3z , |
| unii-9647fm7y3z |
| D10319 |
| panobinostat (usan/inn) |
| (e)-n-hydroxy-3-(4-(((2-(2-methyl-1h-indol-3-yl)ethyl)amino)methyl)phenyl)acrylamide |
| LBH589 - PANOBINOSTAT |
| BCP9000844 |
| BCPP000187 |
| lbh58,9nvp-lbh589,panobinostat |
| CS-0267 |
| n-hydroxy-3-[4-[2-(2-methyl-1h-indol-3-yl)ethylaminomethyl]phenyl]-2(e)-propenamide |
| S1030 |
| panobinostat [who-dd] |
| panobinostat [mart.] |
| panobinostat [inn] |
| panobinostat [mi] |
| panobinostat [usan] |
| (2e)-n-hydroxy-3-[4-({[2-(2-methyl-1h-indol-3-yl)ethyl]amino}methyl)phenyl]prop-2-enamide |
| (e)-n-hydroxy-3-(4-{[2-(2-methyl-1h-indol-3-yl)-ethylamino]-methyl}-phenyl)-acrylamide |
| CCG-208762 |
| MLS006011216 |
| smr004702978 |
| (e)-n-hydroxy-3-(4-((2-(2-methyl-1h-indol-3-yl)ethylamino)methyl)phenyl)acrylamide |
| AM808102 |
| 2-propenamide, n-hydroxy-3-[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2e)- |
| FPOHNWQLNRZRFC-ZHACJKMWSA-N |
| n-hydroxy-3 -[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-2e-2-propenamide |
| n-hydroxy-3-[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-2e-2-propenamide |
| SCHEMBL183197 |
| SCHEMBL164801 |
| gtpl7489 |
| (e)-3-[4-[[2-(2-methyl-1h-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enehydroxamic acid |
| nvp-lbh 589 |
| AC-28652 |
| mfcd09833242 |
| (2e)-n-hydroxy-3-[4-({[2-(2-methyl-1h-indol-3-yl)ethyl]amino}methyl)phenyl]acrylamide |
| DB06603 |
| J-523585 |
| DTXSID40193506 , |
| EX-A169 |
| CHEBI:93774 |
| bdbm198124 |
| (2e)-n-hydroxy-3-[4-[[[2-(2-methyl-1h-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide |
| NCGC00263117-07 |
| SW219369-1 |
| panobinostat(lbh589) |
| n-hydroxy-3-[4-[[2-(2-methyl-1h-indol-3-yl)ethylamino]methyl]phenyl]-2-propenamide |
| 404950-80-7 (free base) |
| AS-17046 |
| BCP01816 |
| Q7131441 |
| NCGC00263117-05 |
| nsc761190 |
| nsc-761190 |
| (lbh-589) |
| SCHEMBL22773814 |
| dtxcid10115997 |
| panobinostatum |
| l01xx42 |
| (2e)-n-hydroxy-3-(4-(((2-(2-methyl-1h-indol-3-yl)ethyl)amino)methyl)phenyl)prop-2-enamide |
| (2e)-n-hydroxy-3-(4-(((2-(2-methyl-1h-indol-3-yl)ethyl)amino)methyl)phenyl)acrylamide |
| panobinostat (mart.) |
| EN300-7395075 |
Panobinostat is an oral pan histone-deacetylase inhibitor used in the treatment of relapsed and refractory multiple myeloma. It modulates the expression of oncogenic and immune-mediating genes involved in tumour cell growth and survival.
Panobinostat (LBH589) has been identified as a potential therapeutic agent for ALL with t(4;11) Studies suggest that the antineoplastic effects are associated with reduced MLL-AF4 fusion protein and reduced expression of HOX genes.
Panobinostat can cause apoptosis induction in refractory metastatic neuroblastoma in combination with MIBG therapy and chemotherapy. It was shown to inhibit CYP2D6 activity in vitro; thus understanding the magnitude of the potential clinical inhibition becomes important.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Panobinostat can cause apoptosis induction in refractory metastatic neuroblastoma in combination with MIBG therapy and chemotherapy." | ( Successful treatment of refractory metastatic neuroblastoma with panobinostat in combination with chemotherapy agents and iodine-131-meta-iodobenzylguanidine therapy. Bordbar, M; Shahriari, M; Shakibazad, N; Zareifar, S; Zekavat, OR, 2020) | 2.24 |
| "Panobinostat was shown to inhibit CYP2D6 activity in vitro; thus understanding the magnitude of the potential clinical inhibition of panobinostat on co-medications that are CYP2D6 substrates becomes important." | ( A clinical investigation of inhibitory effect of panobinostat on CYP2D6 substrate in patients with advanced cancer. Beck, JT; Feld, R; Gazi, L; Hengelage, T; Leighl, N; Nayak, A; Porro, MG; Shepherd, FA; Woo, MM; Zhao, L, 2013) | 1.37 |
Panobinostat treatment reduced cell growth and diminished cell viability, as shown by the induced cell cycle arrest and apoptosis in vitro. Treatment also increased the proapoptotic BIK, BIM, BAX, and BAK levels, as well as increased the activity of caspase-7.
The addition of panobinostat to bortezomib and dexamethasone has demonstrated response and progression-free survival benefits. The incidence and severity of adverse events associated with it can create a challenge for clinicians and patients.
Hepatic impairment did not alter panobinostat absorption with Tmax unchanged at 2 h. Using predictive physiologically-based pharmacokinetic (PBPK) models in the evaluation of the PK of alectinib,. ruxolitinib, and panobinstat exposures can help in using optimal doses with lower toxicity in these populations.
Panobinostat is a histone deacetylase inhibitor that has shown synergistic preclinical anti-myeloma activity when combined with other agents.
Panobinostat has demonstrated potent activity in multiple malignancies, including pediatric brain tumors such as DIPG. The study aimed to determine the influence of food on the oral bioavailability of panobinostats.
The results from these studies were incorporated into the Food and Drug Administration-approved product label. Everolimus 5 mg PO daily and panobinostat 10 mgPO 3 times weekly was the recommended phase II dosing based on their maximum tolerated dose. Simulation using a compartmental BBB model suggests inadequate exposure of free panobinstat in the brain following a recommended oral dosing regimen.
| Role | Description |
|---|---|
| EC 3.5.1.98 (histone deacetylase) inhibitor | An EC 3.5.1.* (non-peptide linear amide C-N hydrolase) inhibitor that interferes with the function of histone deacetylase (EC 3.5.1.98). |
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| angiogenesis modulating agent | An agent that modulates the physiologic angiogenesis process. This is accomplished by endogenous angiogenic proteins and a variety of other chemicals and pharmaceutical agents. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| hydroxamic acid | A compound, RkE(=O)lNHOH, derived from an oxoacid RkE(=O)l(OH) (l =/= 0) by replacing -OH with -NHOH, and derivatives thereof. Specific examples of hydroxamic acids are preferably named as N-hydroxy amides. |
| cinnamamides | An enamide which is cinnamamide or a derivative of cinnamamide obtained by replacement of one or more of its hydrogens. |
| secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
| methylindole | Any member of the class of indoles carrying one or more methyl substituents. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 0.0930 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 0.0930 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 4.4668 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Histone deacetylase 3 | Homo sapiens (human) | EC50 (µMol) | 0.1695 | 0.0300 | 1.8512 | 6.7000 | AID1312869 |
| Protein Tat | HIV-1 M:B_HXB2R | EC50 (µMol) | 0.1300 | 0.1300 | 3.5100 | 8.1000 | AID1598103 |
| Histone deacetylase 1 | Homo sapiens (human) | EC50 (µMol) | 0.1695 | 0.0300 | 1.9877 | 6.7000 | AID1312869 |
| Histone deacetylase 2 | Homo sapiens (human) | EC50 (µMol) | 0.1695 | 0.0300 | 1.8575 | 6.7000 | AID1312869 |
| Histone deacetylase 6 | Homo sapiens (human) | EC50 (µMol) | 0.1507 | 0.0052 | 1.5998 | 6.7000 | AID1312868 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1801572 | In-vitro HDAC Enzymatic Endpoint Assay from Article 10.1021/acschembio.5b00640: \\An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in u00DF-Cell Protection.\\ | 2016 | ACS chemical biology, Feb-19, Volume: 11, Issue:2 | An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. |
| AID1799021 | pfHDAC-1 Enzyme Assay from Article 10.1021/jm801654y: \\Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.\\ | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1236441 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1702237 | Oral bioavailability in Balb/c mouse at 50 mg/kg measured up to 24 hrs by LC/MS/MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma. |
| AID446342 | AUC (0 to infinity) in CD1 mouse at 5 mg/kg, iv | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors. |
| AID1313935 | Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1313947 | Inhibition of human recombinant HDAC6 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1421928 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1312927 | Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of acetylated alpha-tubulin level after 6 hrs by Western blot method | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1431805 | Inhibition of human KDAC3 using FITC-labeled p53 acetylated peptide as substrate after 60 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1210340 | Activity of recombinant human CYP2B6 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1676588 | Binding affinity to Zinc ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID619049 | Competitive inhibition of HDAC4 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1548745 | Inhibition of recombinant HDAC6 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1548756 | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 90 mins | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1591852 | Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system at 1000 nM using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay relative to cont | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1236478 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay in presence of melarsoprol | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1676590 | Binding affinity to Nickel cation assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1545759 | Inhibition of HDAC (unknown origin) | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Indole: A privileged scaffold for the design of anti-cancer agents. |
| AID1189851 | Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Hydroxamic acids block replication of hepatitis C virus. |
| AID1421929 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1548939 | Cmax in BALB/c mouse at 50 mg/kg, po via gavage after 24 hrs by Lc-MS/MS analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1399811 | Solubility in pH 7.4 phosphate buffer solution at 100 uM after 24 hrs by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1548741 | Inhibition of recombinant HDAC4 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1600733 | Antiproliferative activity against human CAL27 cells after 72 hrs by microplate reader based MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1821217 | Antitumor activity against human MV4-11 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 4 mg/kg, ip administered for 24 days | |||
| AID1371033 | Inhibition of recombinant HDAC1 in recombinant Plasmodium falciparum at 1 uM using Ac-RGK(Ac)-AMC fluorogenic peptide as substrate preincubated for 1 hr followed by substrate addition measured after 10 min by fluorescence assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID1399813 | Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1313942 | Inhibition full length human recombinant HDAC3 expressed in baculovirus using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1686358 | Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 48 hrs by Cell-titer-blue cell viability assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia. |
| AID1548942 | Oral bioavailability in BALB/c mouse at 50 mg/kg dosed via gavage after 24 hrs by Lc-MS/MS analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1282299 | Inhibition of HDAC1/2/3 in human HCT116 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1775572 | Inhibition of HDAC in human MM1.S cells assessed as increase in H3K9Ac at > 500 nM after 48 hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID1821220 | Drug uptake in BALB/c mouse xenografted with human AML MV4-11 cells assessed as tumor tissue at 4mg/kg, po measured after 0.5 to 6 hrs by LC-MS/MS | |||
| AID1399834 | Selectivity ratio of Ki for human recombinant SIRT3 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1236447 | Inhibition of human HDAC5 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1236461 | Tmax in po dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1421927 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum Dd2 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1371053 | Antitrypanosomal activity against Trypanosoma brucei brucei measured after 22 hrs by fluorescence-based Alamar blue viability assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID496806 | Inhibition of human HDAC6 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1542187 | Inhibition of HDAC9 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1282244 | Inhibition of recombinant HDAC10 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1559865 | Antitumor activity against human HT-29 cells xenografted in nude mouse assessed as relative tumor volume at 50 mg/kg, po qd for 21 days relative to control (Rvb = 16.68 +/- 5.10 No_unit) | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1676600 | Binding affinity to zinc ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1431806 | Inhibition of human KDAC1 using substrate A after 60 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1210348 | Activity of recombinant human CYP2A6 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1591856 | Inhibition of wild-type human N-terminal GST-tagged CDK2/cycA2 expressed in Sf21 insect cells using FAM-labelled substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1559803 | Inhibition of recombinant His6/GST-tagged human HDAC3 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1676599 | Binding affinity to cupric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1559812 | Inhibition of recombinant human His6/GST-tagged HDAC8 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1548728 | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr fo | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1431818 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1399826 | Inhibition of human recombinant SIRT3 using fluoro-lysine sirtuin 2 deacetylase substrate after 45 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1821190 | Half life in CD-1 mouse at 50 mg/kg, po measured upto 24 hrs | |||
| AID1548764 | Inhibition of HDAC6 in human MV4-11 cells assessed as tubulin acetylation at 500 nM incubated for 3 hrs followed by compound washout and measured after 30 mins by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1559817 | Inhibition of recombinant human N-terminal GST-tagged SIRT2 expressed in Escherichia coli using Ac-Arg-His-Lys-Lys(Ac)-AMC as susbtrate after 2 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1591857 | Antiproliferative activity against human A549 cells measured after 72 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1600732 | Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and further incubation for 3 hrs by microplate reader based fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1676591 | Binding affinity to Nickel cation assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1821246 | Drug distribution in BALB/c mouse liver measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID1431812 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1399824 | Inhibition of human recombinant SIRT1 using fluorogenic HDAC substrate after 20 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1598093 | Cytotoxicity against human HepG2 cells assessed as reduction in cell growth incubated for 48 hrs by CellTiter-Glo assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1282300 | Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1312916 | Cytotoxicity against human HBL1 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1312866 | Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1210324 | Activity of recombinant human CYP3A5 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1845902 | Reversal of HIV-1 latency infected in human U1 cells assessed as fold increase in p24 expression level at 31.1 nM incubated for 48 hrs by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID1845914 | Inhibition of HIV-1 latency in human CD4+ve Th cells infected NL4.3-Luc virus assessed as p24 expression level incubated for 48 hrs by v450 dye based flow cytometry | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID414980 | Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. |
| AID1236466 | Half-life in iv dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1676598 | Binding affinity to cupric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1525777 | Inhibition of HADC1 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. |
| AID1821197 | Inhibition of human recombinant HDAC5 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID1821202 | Inhibition of human recombinant HDAC11 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID1282243 | Inhibition of recombinant HDAC9 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1399809 | Clearance in human hepatocytes assessed per million cells at 1 uM after 5 to 90 mins by LC-MS/MS analysis | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1236470 | Trypanocidal activity against Trypanosoma brucei brucei assessed as killing of parasite densities of 10'4 to 10'6 cells/ml at 2.8 uM after 16 hrs by clonal dilution method | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1210350 | Activity of recombinant human CYP2C8 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1312895 | Toxicity in NOD/SCID mouse xenografted with human MM1S cells assessed as mortality at 10 mg/kg, ip administered every 2 days for 6 days | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1676596 | Binding affinity to Ferric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1600735 | Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and further incubation for 3 hrs by microplate reader based fluorescence assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1821234 | Antitumor activity against human MV4-11 cells xenografted in balb/c mouse assessed as increase accumulation of AcHH4 protein level at 4 mg/kg, ip measured after 8 hrs relative to control | |||
| AID1775552 | Inhibition of recombinant HDAC6 (unknown origin) | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID1127840 | Cytotoxicity against human M14 cells assessed as cell viability after 24 hrs using GF-AFC as substrate by ApoTox-Glo triplex assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID1210354 | Activity of recombinant human CYP2C18 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1399835 | Selectivity ratio of Ki for human recombinant SIRT7 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1421922 | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1591858 | Antiproliferative activity against human HepG2 cells measured after 72 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1236449 | Inhibition of human HDAC9 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1312849 | Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1775569 | Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation measured up to 72 hrs by CellTiter96 Aqueous one reagent based assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID1313950 | Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID496801 | Inhibition of human HDAC1 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID446345 | Clearance in CD1 mouse at 15 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors. |
| AID1559804 | Inhibition of recombinant His6/GST-tagged human HDAC6 expressed in baculovirus infected High5 insect cells using Boc-Lys(epsion-acetyl)-AMC as substrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1845899 | Reversal of HIV-1 latency infected in human U1 cells assessed as fold increase in p24 expression level at 15.6 nM incubated for 48 hrs by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID1282282 | Antitumor activity against human Ramos cells xenografted in NOD/SCID mouse assessed as tumor mass change at 10 mg/kg, ip q2d for 6 days | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1821249 | Drug distribution in BALB/c mouse heart measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID1312919 | Cytotoxicity against human SUDHL4 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID618092 | Toxicity in nude BALB/c mouse xenografted with human HCT116 cells assessed as body weight loss at 50 mg/kg, po QD for 21 days measured on day 12 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1821193 | AUC (0 to infinity) in CD-1 mouse at 50 mg/kg, po measured upto 24 hrs | |||
| AID1821221 | Drug uptake in BALB/c mouse xenografted with human AML MV4-11 cells assessed as tumor tissue at 4 mg/kg ip measured after 0.5 to 6 hrs by LC-MS/MS | |||
| AID1313940 | Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1676597 | Binding affinity to cupric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1282230 | Inhibition of human recombinant HDAC6 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID446346 | Volume of distribution at steady state in CD1 mouse at 15 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors. |
| AID1236448 | Inhibition of human HDAC7 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID748113 | Inhibition of HDAC2 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1846017 | Anticancer activity against human UW426 cells assessed as reduction in cell viability incubated for 72 hrs by CCK assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID1312868 | Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1600726 | Selectivity index, ratio of IC50 for C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in insect cells to IC50 for C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Ba | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1548755 | Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 10 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1236453 | Cmax in po dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1542189 | Inhibition of HDAC11 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1210356 | Activity of recombinant human CYP2C19 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1421926 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum 3D7 infected in human erythrocytes | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1236467 | Half-life in po dosed human measured under phase 2 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1676601 | Binding affinity to Zinc ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID748109 | Inhibition of HDAC6 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1821238 | Drug distribution in BALB/c mouse spleen measured at 4 mg/kg, po or ip after 0.5 hrs | |||
| AID1882467 | Inhibition of HDAC8 (unknown origin) | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology. |
| AID1846016 | Anticancer activity against human UW228 cells assessed as reduction in cell viability incubated for 72 hrs by CCK assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID1431817 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1559810 | Inhibition of recombinant N-terminal GST-tagged full length human HDAC5 expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1312861 | Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1210352 | Activity of recombinant human CYP2C9 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1548759 | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 10 mins | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1399821 | Inhibition of human recombinant HDAC9 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1589102 | Potency index, ratio of IC50 for BnNHC to IC50 for test compound for inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID750109 | Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | Design, synthesis and biological evaluation of indeno[1,2-d]thiazole derivatives as potent histone deacetylase inhibitors. |
| AID1559814 | Inhibition of recombinant human His6/GST-tagged HDAC10 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1282288 | Toxicity in Balb/c nude mouse xenografted with human HCT116 cells assessed as change in body weight at 10 mg/kg, ip q2d for 6 days | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1542180 | Inhibition of HDAC2 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1371080 | Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID1559809 | Inhibition of recombinant human His6/GST-tagged HDAC4 expressed in baculovirus infected High5 insect cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1236457 | AUC in po dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1548737 | Inhibition of recombinant HDAC1 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1591855 | Inhibition of wild-type human N-terminal GST-tagged CDK2/cycA2 expressed in Sf21 insect cells at 100 nM using FAM-labelled substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay relative to contr | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1312914 | Cytotoxicity against human MM1S cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1559854 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1399832 | Selectivity ratio of Ki for human recombinant SIRT1 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID619043 | Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1236462 | Tmax in iv dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1548274 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay | |||
| AID1548757 | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1236459 | AUC in po dosed human measured under phase 2 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1548744 | Inhibition of recombinant HDAC9 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1821241 | Drug distribution in BALB/c mouse gut measured at 4 mg/kg, po or ip after 0.5 hrs after 0.5 hrs | |||
| AID1785449 | Inhibition of HDAC1 (unknown origin) using Ac-peptide-AMC as substrate incubated for 1 hr by fluorescence method | |||
| AID1441630 | Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA preincubated for 10 mins followed by substrate addition measured after 10 mins | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1591853 | Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1542183 | Inhibition of HDAC5 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1126987 | Inhibition of HDAC2 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity. |
| AID1676595 | Binding affinity to Ferric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1236443 | Inhibition of human HDAC2 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1399816 | Inhibition of human recombinant HDAC3 using fluorogenic HDAC substrate after 10 mins by spectrophotometric method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1312853 | Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1821195 | Oral bioavailability in CD-1 mouse at 50 mg/kg measured upto 24 hrs | |||
| AID1312852 | Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1431811 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1210332 | Activity of recombinant human CYP2D6 expressed in supersomes assessed as enzyme-mediated drug metabolism measured as compound remaining at 10 uM after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1542182 | Inhibition of HDAC4 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1589104 | Potency index, ratio of IC50 for belinostat-1 to IC50 for test compound for inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID1399810 | Solubility in PG/EtOH (96%) at 30 mg/mL after 24 hrs by UV-spectrometric method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1548933 | Mutagenecity in Salmonella typhimurium TA100 at 10 uM in presence of S9 liver homogenate after 2 to 3 days by mini-Ames test | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1441699 | Inhibition of recombinant human LTA4H aminopeptidase activity expressed in Escherichia coli BL21 (DE3) pLysS assessed as formation of p-NA from Ala-p-NA at 10 uM preincubated for 10 mins followed by substrate addition measured after 10 mins | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1431804 | Inhibition of human KDAC6 using FITC-labeled histone H4 acetylated peptide as substrate after 60 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1441631 | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1542179 | Inhibition of HDAC1 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID619051 | Competitive inhibition of HDAC6 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1236458 | AUC in iv dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1821250 | Drug distribution in BALB/c mouse brain measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID1821247 | Drug distribution in BALB/c mouse kidney measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID1821235 | Antitumor activity against human MV4-11 cells xenografted in balb/c mouse assessed as increase in accumulation of AcHH3 protein level at 4 mg/kg, ip measured after 8 hrs relative to control | |||
| AID1548738 | Inhibition of recombinant HDAC2 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1598139 | Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as maximum LTR activity at 0.1 uM incubated for 48 hr by FACSCalibur flow cytometry relative to control | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1321704 | Inhibition of recombinant HDAC1 (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease. |
| AID1312888 | Antitumor activity against human MM1S cells xenografted in NOD/SCID mouse assessed as change in tumor mass at 10 mg/kg, ip administered every 2 days for 6 days measured every 2 days of compound dosing relative to control | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1371081 | Selectivity index, ratio of IC50 for human NFF cells to IC50 for Plasmodium falciparum | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID1399827 | Inhibition of SIRT7 (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1600734 | Antiproliferative activity against human A2780 cells after 72 hrs by microplate reader based MTT assay | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1282302 | Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1558024 | Induction of apoptosis in mouse SM1 cells at 100 nM by caspase3/7 reagent based luminescence assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models. |
| AID1282242 | Inhibition of recombinant HDAC7 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID748111 | Inhibition of HDAC4 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID748112 | Inhibition of HDAC3 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1312859 | Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1282238 | Inhibition of recombinant HDAC2 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1236454 | Cmax in iv dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1542184 | Inhibition of HDAC6 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1602601 | Cytotoxicity against mouse KPC monolayer cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5 | Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer. |
| AID748110 | Inhibition of HDAC5 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1312918 | Cytotoxicity against human Raji cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1312915 | Cytotoxicity against human OCI-LY1 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1312909 | Toxicity in NOD/SCID mouse xenografted with human MM1S cells assessed as body weight loss at 10 mg/kg, ip administered every 2 days for 6 days measured on day 12 post last dose | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1210326 | Activity of recombinant human CYP4A11 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1399815 | Inhibition of human recombinant HDAC2 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1431814 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1127852 | Induction of apoptosis human M14 cells assessed as caspase activity at 100 uM after 4 hrs using DEVD peptide as substrate by ApoTox-Glo triplex assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID1600729 | Inhibition of N-terminal GST-tagged recombinant human HDAC6 (1 to 1215 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins me | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1282245 | Inhibition of recombinant HDAC11 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1236450 | Inhibition of human HDAC6 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID748106 | Inhibition of HDAC8 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1312869 | Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1210338 | Inhibition of HDAC6 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID619044 | Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1282231 | Inhibition of human recombinant HDAC8 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1821216 | Antitumor activity against human MV4-11 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 2 to 4 mg/kg, po administered for 24 days | |||
| AID1598133 | Selectivity ratio of EC50 for activation of non-specific gene expression in HEK293- FlpIn-FM cells harboring LTR driven CBR reporter co-expressing CMV driven CBG reporter assessed as CMV driven gene expression to EC50 for activation of Tat-mediated HIV1 t | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1559808 | Inhibition of recombinant human His6/GST-tagged HDAC2 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1210346 | Activity of recombinant human CYP1B1 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1559868 | Antitumor activity against human HT-29 cells xenografted in nude mouse assessed as reduction in tumor growth at 50 mg/kg, po qd for 21 days relative to control | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1785450 | Inhibition of HDAC6 (unknown origin) using Ac-peptide-AMC as substrate incubated for 1 hr by fluorescence method | |||
| AID1189850 | Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay | 2015 | Journal of medicinal chemistry, Jan-22, Volume: 58, Issue:2 | Hydroxamic acids block replication of hepatitis C virus. |
| AID1845900 | Reversal of HIV-1 latency infected in human ACH-2 cells assessed as fold increase in p24 expression level at 15.6 nM incubated for 48 hrs by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID1559852 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1882462 | Inhibition of HDAC6 (unknown origin) | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology. |
| AID1127841 | Induction of apoptosis human M14 cells assessed as caspase activity after 24 to 48 hrs using DEVD peptide as substrate by ApoTox-Glo triplex assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID1210339 | Inhibition of his-strep-tagged HDAC8 (unknown origin) expressed in SF9 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1210318 | Activity of recombinant human CYP2E1 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1312906 | Toxicity in NOD/SCID mouse xenografted with human Ramos cells assessed as body weight loss at 10 mg/kg, ip administered every 2 days for 6 days measured on day 7 post last dose | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID619045 | Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID708192 | Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. |
| AID1821239 | Drug distribution in BALB/c mouse liver measured at 4 mg/kg, po or ip after 0.5 hrs after 0.5 hrs | |||
| AID619048 | Competitive inhibition of HDAC3 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1210316 | Activity of recombinant human CYP2D6 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1312912 | Cytotoxicity against human U266 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID496809 | Inhibition of human HDAC9 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1210328 | Drug metabolism in Escherichia coli JM109 assessed as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID619046 | Competitive inhibition of HDAC1 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1821198 | Inhibition of human recombinant HDAC7 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID496805 | Inhibition of human HDAC5 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1882260 | Inhibition of HDAC6 (unknown origin) | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | A review on the treatment of multiple myeloma with small molecular agents in the past five years. |
| AID1882456 | Inhibition of HDAC1 (unknown origin) | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology. |
| AID1321705 | Inhibition of recombinant HDAC2 (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease. |
| AID1236445 | Inhibition of human HDAC8 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1559862 | Antitumor activity against human HT-29 cells xenografted in nude mouse assessed as tumor volume at 50 mg/kg, po qd for 21 days measured on day 21 (Rvb = 2854 +/- 940 mm3) | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1312865 | Inhibition of His-tagged full length recombinant human p110gamma expressed in baculovirus expression system incubated for 1 hr by ADP-gloreagen assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID620532 | Reactivation of MeCp2 mutant expression in human GM11272 cells at 1 to 100 nM by PCR method | 2011 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18 | Clonal Rett Syndrome cell lines to test compounds for activation of wild-type MeCP2 expression. |
| AID1282239 | Inhibition of recombinant HDAC3 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1548727 | Inhibition of recombinant human HDAC2 expressed in baculovirus expression system using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1559859 | Antitumor activity against azoxymethane-induced colitis-associated cancer C57BL/6 mouse model assessed as tumor incidence at 50 mg/kg, po via gavage administered with AOM followed by 3 cycles of 2.5% DSS given in water for 5 days and compound administered | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1821248 | Drug distribution in BALB/c mouse gut measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID1548276 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells assessed combination index in presence of bortezomib at 1:1 compound to bortezomib ratio incubated for 48 hrs by MTT assay | |||
| AID1589101 | Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID1441632 | Binding affinity to recombinant human LTA4H hydrolase assessed as change in melting temperature at 50 uM by SYPRO orange dye-based thermofluor assay | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1845901 | Reversal of HIV-1 latency infected in human ACH-2 cells assessed as fold increase in p24 expression level at 31.1 nM incubated for 48 hrs by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | HIV latency reversal agents: A potential path for functional cure? |
| AID1431822 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1210336 | Inhibition of HDAC3 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1431815 | Selectivity ratio of IC50 for human KDAC1 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1600730 | Inhibition of C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1559811 | Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as susbtrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1313945 | Inhibition of N-terminal GST-tagged and C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues ) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1723749 | Inhibition of human recombinant HDAC4 using Boc-Lys-(epsilon-Tfa)-AMC fluorogenic substrate incubated for 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18 | Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups. |
| AID1236444 | Inhibition of human HDAC3 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1210322 | Activity of recombinant human CYP3A4 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis in presence of cytochrome b5 | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1424834 | Induction of apoptosis in human MV4-11 cells at 30 nM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry | 2018 | European journal of medicinal chemistry, May-25, Volume: 152 | Design and biological evaluation of tetrahydro-β-carboline derivatives as highly potent histone deacetylase 6 (HDAC6) inhibitors. |
| AID414981 | Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine uptake | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum. |
| AID1548762 | Inhibition of class I HDAC in human MV4-11 cells assessed as reduction in histone H3 levels at 500 nM incubated for 3 hrs followed by compound washout and measured after 1 hr by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID619050 | Competitive inhibition of HDAC5 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1559813 | Inhibition of recombinant human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 cells using Ac-Leu-Gly-Lys(Tfa)-AMC as substrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1589107 | Selectivity index, ratio of IC50 for inhibition of human recombinant HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by fluorescence based assay to IC50 for inhibition of human recombinant HDAC1 pre-incubated for 30 mi | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID1371034 | Antimalarial activity against Plasmodium falciparum infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID1598102 | Activation of Tat-mediated HIV1 transcription in HEK293- FlpIn-FM cells harboring LTR driven CBR reporter co-expressing CMV driven CBG reporter assessed as maximum LTR activity at 0.2 uM incubated for 48 hr using Chroma-Glo substrate by luciferase dual re | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1312854 | Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1236465 | Half-life in po dosed human measured under phase 1 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1559856 | Antiproliferative activity against human T47D cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1399829 | Selectivity ratio of Ki for human recombinant HDAC4 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1821222 | Plasma concentration in BALB/c mouse xenografted with human AML MV4-11 cells at 4 mg/kg, po | |||
| AID1525776 | Inhibition of HADC6 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. |
| AID1600727 | Selectivity index, ratio of IC50 for C-terminal His-tagged/N-terminal GST-tagged recombinant human HDAC4 (627 to 1084 residues) expressed in Baculovirus infected insect cells to IC50 for C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) ex | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1321707 | Inhibition of recombinant HDAC6 (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease. |
| AID1399818 | Inhibition of human recombinant HDAC4 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1313946 | Inhibition of N-terminal GST-tagged full length human recombinant HDAC5 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1775549 | Inhibition of recombinant HDAC1 (unknown origin) | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID1542181 | Inhibition of HDAC3 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1548726 | Inhibition of recombinant HDAC1 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1548890 | Induction of apoptosis in human MV4-11 cells harboring wild type p53/FLT3-ITD mutant assessed as cleavage of pro-caspase 3 at 100 nM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1600728 | Inhibition of C-terminal His-fusion tagged/N-terminal Strep-2 tagged recombinant human HDAC8 (1 to 377 residues) expressed in insect cells using Boc-Lys(TFa)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation fo | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1210330 | Activity of recombinant human CYP3A4 expressed in supersomes assessed as enzyme-mediated drug metabolism measured as compound remaining at 10 uM after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1816688 | Inhibition of HDAC5 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer. |
| AID1821187 | Cmax in CD-1 mouse at 50 mg/kg, po measured upto 24 hrs | |||
| AID1821243 | Drug distribution in BALB/c mouse brain measured at 4 mg/kg, po or ip after 0.5 hrs after 0.5 hrs | |||
| AID1821196 | Inhibition of human recombinant HDAC4 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID1548941 | AUC (0 to infinity) in BALB/c mouse at 50 mg/kg, po via gavage after 24 hrs by Lc-MS/MS analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID619042 | Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1371032 | Inhibition of HDAC1 in Plasmodium falciparum 3D7 nuclear extract using Ac-RGK(Ac)-AMC fluorogenic peptide as substrate preincubated for 1 hr followed by substrate addition measured after 10 min by fluorescence assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID619047 | Competitive inhibition of HDAC2 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1821240 | Drug distribution in BALB/c mouse kidney measured at 4 mg/kg, po or ip after 0.5 hrs after 0.5 hrs | |||
| AID1559855 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1676589 | Binding affinity to Nickel cation assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1312881 | Antitumor activity against human Ramos cells xenografted in NOD/SCID mouse assessed as change in tumor mass at 10 mg/kg, ip administered every 2 days for 6 days measured every 2 days of compound dosing relative to control | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1446915 | Inhibition of Schistosoma mansoni KDAC8 using (FAM)-labeled peptide as substrate after 60 mins by microfluidic assay | 2017 | Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7 | Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy. |
| AID1371079 | Cytotoxicity against human NFF cells after 72 hrs by SRB assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID1821201 | Inhibition of human recombinant HDAC10 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID1821218 | Antitumor activity against human MV4-11 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 4 mg/kg, po administered for 24 days | |||
| AID1312850 | Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1431803 | Inhibition of human KDAC8 after 60 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1548940 | Half life in BALB/c mouse at 50 mg/kg, po via gavage after 24 hrs by Lc-MS/MS analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1126989 | Inhibition of HDAC6 in human U937 cells assessed as increase of intracellular acetylated alpha-tubulin level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity. |
| AID619161 | Oral bioavailability in nude BALB/c mouse at 50 mg/kg | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1399817 | Inhibition of human recombinant HDAC8 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1548758 | Inhibition of recombinant human C-terminal GST/His-tagged HDAC3 (1 to 428 residues) co-expressed with human N-terminal GST-tagged NCOR2 (395 to 489 residues) in baculovirus infected Sf9 cells using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1548915 | Induction of apoptosis in human RS4:11 cells harboring wild type p53/FLT3 assessed as cleavage of pro-caspase 3 at 100 nM after 24 hrs by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1236446 | Inhibition of human HDAC4 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1312856 | Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1548742 | Inhibition of recombinant HDAC5 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1313948 | Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID1312860 | Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1548753 | Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 60 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1589103 | Potency index, ratio of IC50 for panobinostat to IC50 for test compound for inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID1399812 | Inhibition of human recombinant HDAC1 using Fluor de Lys as substrate after 2 hrs by fluorescence method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1548740 | Inhibition of recombinant HDAC8 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1821200 | Inhibition of human recombinant HDAC9 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID1821260 | Drug distribution in tumor of BALB/c mouse xenografted with human MV4-11 cells assessed as measured after 8 hrs | |||
| AID1210342 | Activity of recombinant human CYP1A1 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID639364 | Clearance in mouse | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
| AID1399833 | Selectivity ratio of Ki for human recombinant SIRT2 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID618329 | Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 21 days measured on day 15 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1312847 | Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1312858 | Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1312923 | Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of acetylated histone H3 level after 6 hrs by Western blot method | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1559857 | Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1548729 | Inhibition of recombinant HDAC6 (unknown origin) using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based micro plate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1548743 | Inhibition of recombinant HDAC7 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1775571 | Permeability of the compound in PBS/EtOH buffer (70:30) incubated for 18 hrs by UV plate reader based PAMPA assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID1431816 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1126986 | Inhibition of HDAC1 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity. |
| AID446347 | Oral bioavailability in CD1 mouse at 15 mg/kg | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors. |
| AID619041 | Inhibition of full length recombinant HDAC1 using Fluor de Lys as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1542188 | Inhibition of HDAC10 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1399819 | Inhibition of human recombinant HDAC5 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1589106 | Inhibition of human recombinant HDAC2 pre-incubated for 30 mins before substrate addition and measured after 30 mins by fluorescence based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID1282240 | Inhibition of recombinant HDAC4 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1421924 | Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1312928 | Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of acetylated alpha-tubulin level after 6 hrs by Western blot method | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1559816 | Inhibition of recombinant human N-terminal GST-tagged SIRT1 expressed in Escherichia coli using Ac-Arg-His-Lys-Lys(Ac)-AMC as susbtrate after 1 hr by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1431821 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1421925 | Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1548763 | Inhibition of class I HDAC in human MV4-11 cells assessed as reduction in histone H3 levels at 500 nM incubated for 3 hrs followed by compound washout and measured after 6 hr by Western blot analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1462230 | Inhibition of BRD4 (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17 | Structure-based design, synthesis and in vitro antiproliferative effects studies of novel dual BRD4/HDAC inhibitors. |
| AID619056 | Competitive inhibition of HDAC11 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1399814 | Inhibition of human recombinant HDAC1 using fluorogenic HDAC substrate after 15 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1591854 | Inhibition of wild-type human N-terminal GST-tagged CDK2/cycA2 expressed in Sf21 insect cells at 10 nM using FAM-labelled substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay relative to contro | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1775551 | Inhibition of recombinant HDAC3 (unknown origin) | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID619054 | Competitive inhibition of HDAC9 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1441700 | Inhibition of recombinant human LTA4H Epoxide Hydrolase expressed in Escherichia coli BL21 (DE3) pLysS at 10 uM preincubated for 10 mins followed by addition of LTA4 as substrate measured after 15 mins by reverse-phase HPLC analysis | 2017 | Journal of medicinal chemistry, 03-09, Volume: 60, Issue:5 | Drug Repurposing of Histone Deacetylase Inhibitors That Alleviate Neutrophilic Inflammation in Acute Lung Injury and Idiopathic Pulmonary Fibrosis via Inhibiting Leukotriene A4 Hydrolase and Blocking LTB4 Biosynthesis. |
| AID1431819 | Selectivity ratio of IC50 for human KDAC3 to IC50 for human KDAC8 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1775570 | Cytotoxicity against human THLE-2 cells assessed as decrease in cell viability measured after 72 hrs by Vialight-plus cell proliferation assay | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID1399830 | Selectivity ratio of Ki for human recombinant HDAC7 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1821223 | Plasma concentration in BALB/c mouse xenografted with human AML MV4-11 cells at 4 mg/kg, ip | |||
| AID1127853 | Cytotoxicity against human M14 cells assessed as cell viability at 100 uM after 4 hrs using GF-AFC as substrate by ApoTox-Glo triplex assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID496803 | Inhibition of human HDAC3 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1821244 | Drug distribution in BALB/c mouse lung measured at 4 mg/kg, po or ip after 0.5 hrs after 0.5 hrs | |||
| AID1600731 | Inhibition of C-terminal GST-tagged recombinant human HDAC2 (1 to 488 residues) expressed in Baculovirus infected insect cells using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and further incubation for 90 mins mea | 2019 | Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19 | Novel α,β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. |
| AID1558023 | Cytotoxicity against mouse SM1 cells at 100 nM by ApoTox-Glo triplex assay | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 | Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models. |
| AID1591851 | Inhibition of recombinant human full-length C-terminal FLAG-tagged HDAC1 expressed in baculovirus expression system at 10 nM using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay relative to contro | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1525779 | Inhibition of HADC3 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. |
| AID1821259 | Drug distribution in tumor of BALB/c mouse xenografted with human MV4-11 cells assessed as measured after 2 hrs | |||
| AID1312917 | Cytotoxicity against human Ramos cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1559815 | Inhibition of recombinant human His6/GST-tagged HDAC11 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as susbtrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1559905 | Toxicity in nude mouse xenografted with human HT-29 cells assessed as body weight at 50 mg/kg, po qd for 21 days measured on day 21 (Rvb = 19.1 gms) | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1282229 | Inhibition of human recombinant HDAC1 using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1127851 | Cytotoxicity against human M14 cells assessed as cell viability at 100 uM after 4 hrs using bis-AAF-R110 as substrate by ApoTox-Glo triplex assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis. |
| AID1236455 | Cmax in po dosed human measured under phase 2 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1598094 | Cytotoxicity against HEK293 cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID748114 | Inhibition of HDAC1 (unknown origin) after 60 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Discovery of the first histone deacetylase 6/8 dual inhibitors. |
| AID1399823 | Inhibition of human recombinant HDAC10 using fluorogenic HDAC substrate after 45 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1371082 | Selectivity index, ratio of IC50 for HEK293 cells to IC50 for Plasmodium falciparum | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12 | Lysine Deacetylase Inhibitors in Parasites: Past, Present, and Future Perspectives. |
| AID1431820 | Selectivity ratio of IC50 for human KDAC8 to IC50 for human KDAC6 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1676593 | Binding affinity to Gallium ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1479839 | Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 30 to 50 nM after 24 hrs by propidium iodide staining-based flow cytometric method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
| AID1321706 | Inhibition of recombinant HDAC3 (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease. |
| AID1676602 | Binding affinity to ferric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1676594 | Binding affinity to gallium ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1282241 | Inhibition of recombinant HDAC5 (unknown origin) using AMC labeled AC-peptide as substrate incubated for 1 hr by fluorescence analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1846018 | Anticancer activity against human MED-MEB-8A cells assessed as reduction in cell viability incubated for 72 hrs by CCK assay | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | Medulloblastoma drugs in development: Current leads, trials and drawbacks. |
| AID1821258 | Drug distribution in tumor of BALB/c mouse xenografted with human MV4-11 cells assessed as measured after 0.5 hrs | |||
| AID1559853 | Antiproliferative activity against human EBC1 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1598104 | Activation of non-specific gene expression in human J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as CMV driven gene expression incubated for 48 hr by FACSCalibur flow cytometry | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1559851 | Antiproliferative activity against human Bel7402 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1548275 | Antiproliferative activity against bortezomib resistant human KM3/BTZ cells in presence of bortezomib incubated for 48 hrs by MTT assay | |||
| AID446344 | Half life in CD1 mouse at 15 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors. |
| AID1399822 | Inhibition of human recombinant HDAC6 using fluorogenic HDAC substrate after 30 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1559858 | Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 72 hrs | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1686371 | Cytotoxicity against human PBMC assessed as reduction in cell viability at 10 nM incubated for 48 hrs by Cell-titer-blue cell viability assay | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | Development of Allosteric Hydrazide-Containing Class I Histone Deacetylase Inhibitors for Use in Acute Myeloid Leukemia. |
| AID1312913 | Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1126988 | Inhibition of HDAC3 in human U937 cells assessed as increase of intracellular acetylated histone H4 level at 1 uM after 24 hrs by Western blot analysis | 2014 | Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8 | Discovery of the first N-hydroxycinnamamide-based histone deacetylase 1/3 dual inhibitors with potent oral antitumor activity. |
| AID496808 | Activity of human HDAC8 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID618098 | Toxicity in nude BALB/c mouse xenografted with human HCT116 cells assessed as mouse survival at 50 mg/kg, po QD for 21 days measured on day 22 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1542185 | Inhibition of HDAC7 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1210335 | Inhibition of flag-tagged HDAC2 (unknown origin) expressed in SF21 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1821199 | Inhibition of human recombinant HDAC8 using Boc-Lys(triflouroacetyI)-AMC substrate incubated for 2 hrs by fluorescence based assay | |||
| AID1559802 | Inhibition of recombinant His6/GST-tagged human HDAC1 expressed in baculovirus infected High5 insect cells using Ac-Lys-Tyr-Lys(epsilon-acetyl)-AMC as substrate after 24 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1548739 | Inhibition of recombinant HDAC3 (unknown origin) | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1548752 | Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 90 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID496807 | Inhibition of human HDAC7 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1479834 | Inhibition of HDAC6 in human MV4-11 cells assessed as induction of alpha-tubulin hyperacetylation at 50 nM after 2 to 24 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
| AID1399831 | Selectivity ratio of Ki for human recombinant HDAC9 to Ki for human recombinant HDAC1 | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1882466 | Inhibition of HDAC3 (unknown origin) | 2022 | Journal of medicinal chemistry, 02-24, Volume: 65, Issue:4 | Chasing a Breath of Fresh Air in Cystic Fibrosis (CF): Therapeutic Potential of Selective HDAC6 Inhibitors to Tackle Multiple Pathways in CF Pathophysiology. |
| AID1210334 | Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1548754 | Inhibition of recombinant human HDAC1 using Boc-Lys(acetyl)-AMC as substrate preincubated for 30 mins followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1763569 | Cytotoxicity against human PANC1 cells assessed as reduction in cell viability incubated upto 72 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents. |
| AID1399820 | Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2a after 45 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1548730 | Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue dye based spectrophotometric analysis | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity. |
| AID1868471 | Inhibition of HIV-1 latency reversal in GFP-fused human J-lat 9.2 cells at 0.1 uM incubated for 24 hrs in presence of pan-PKC inhibitor Go 6983 by flow cytometry analysis | 2022 | Journal of natural products, 05-27, Volume: 85, Issue:5 | Ansellone J, a Potent |
| AID1236477 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay in presence of nifurtimox | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1559818 | Inhibition of recombinant human N-terminal His-tagged SIRT3 expressed in Escherichia coli using Ac-Arg-His-Lys-Lys(Ac)-AMC as susbtrate after 2 hrs by fluorescence based assay | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2 | Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors. |
| AID1598103 | Activation of Tat-mediated HIV1 transcription in J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as LTR-driven gene expression incubated for 48 hr by FACSCalibur flow cytometry | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models. |
| AID1525780 | Inhibition of HADC8 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-09, Volume: 63, Issue:1 | Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases. |
| AID1312864 | Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1210320 | Activity of recombinant human CYP3A4 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1589105 | Inhibition of human recombinant HDAC1 pre-incubated for 30 mins before substrate addition and measured after 30 mins by fluorescence based assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling. |
| AID1821242 | Drug distribution in BALB/c mouse heart measured at 4 mg/kg, po or ip after 0.5 hrs after 0.5 hrs | |||
| AID1210337 | Inhibition of HDAC4 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID619055 | Competitive inhibition of HDAC10 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1821245 | Drug distribution in BALB/c mouse spleen measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID1431813 | Selectivity ratio of IC50 for human KDAC6 to IC50 for human KDAC1 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors. |
| AID1479836 | Induction of HDAC6 degradation in human MV4-11 cells at 50 nM after 24 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8 | Marbostat-100 Defines a New Class of Potent and Selective Antiinflammatory and Antirheumatic Histone Deacetylase 6 Inhibitors. |
| AID639798 | Oral bioavailability in mouse | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Discovery, synthesis, and pharmacological evaluation of spiropiperidine hydroxamic acid based derivatives as structurally novel histone deacetylase (HDAC) inhibitors. |
| AID1312857 | Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1421923 | Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites. |
| AID1236442 | Inhibition of human HDAC1 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1312851 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1591859 | Antiproliferative activity against human CAL148 cells measured after 72 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2. |
| AID1676592 | Binding affinity to Gallium ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors. |
| AID1775550 | Inhibition of recombinant HDAC2 (unknown origin) | 2021 | Journal of medicinal chemistry, 03-25, Volume: 64, Issue:6 | Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with |
| AID496804 | Inhibition of human HDAC4 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1312924 | Inhibition of HDAC1/2/3 in human HCT116 cells assessed as upregulation of acetylated histone H3 level after 6 hrs by Western blot method | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID619052 | Competitive inhibition of HDAC7 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1236476 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay in presence of suramin | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1312867 | Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Leu-Gly-Lys (Ac)-AMC as substrate after 30 mins by fluorescence assay | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1399828 | Inhibition of human recombinant HDAC11 using fluorogenic HDAC substrate class 2a after 30 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1236475 | Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay in presence of pentamidine | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID619053 | Competitive inhibition of HDAC8 using KI-104 as substrate by fluorescence assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1542186 | Inhibition of HDAC8 (unknown origin) | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy. |
| AID1313949 | Inhibition of C-terminal His-tagged full length human recombinant HDAC8 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors. |
| AID496802 | Inhibition of human HDAC2 | 2010 | Nature chemical biology, Mar, Volume: 6, Issue:3 | Chemical phylogenetics of histone deacetylases. |
| AID1312855 | Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat | 2016 | Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11 | Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities. |
| AID1282298 | Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, Feb-25, Volume: 59, Issue:4 | Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. |
| AID1210344 | Activity of recombinant human CYP1A2 expressed in Escherichia coli JM109 co-expressing P450 reductase assessed as enzyme-mediated drug metabolism measured as compound remaining after 1 hr by LC-MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5 | Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589). |
| AID1236463 | Tmax in po dosed human measured under phase 2 trial | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16 | Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT). |
| AID1399825 | Inhibition of human recombinant SIRT2 using fluoro-lysine sirtuin 2 deacetylase substrate after 60 mins by fluorimetrc method | 2018 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17 | Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma. |
| AID1821251 | Drug distribution in BALB/c mouse lung measured at 4 mg/kg, po or ip after 2 to 8 hrs after 0.5 hrs | |||
| AID618261 | Antitumor activity against human HCT116 cells xenografted in nude BALB/c mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 21 days measured on day 18 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. |
| AID1347415 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347414 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1346068 | Human histone deacetylase 8 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346077 | Human histone deacetylase 3 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346090 | Human histone deacetylase 9 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346032 | Human histone deacetylase 6 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346131 | Human histone deacetylase 7 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346134 | Human histone deacetylase 1 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346104 | Human histone deacetylase 4 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1346082 | Human histone deacetylase 2 (3.5.1.- Histone deacetylases (HDACs)) | 2008 | The Biochemical journal, Jan-15, Volume: 409, Issue:2 | Determination of the class and isoform selectivity of small-molecule histone deacetylase inhibitors. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1802011 | HDAC6 fluorescence anisotropy assay from Article 10.1038/nchembio.2134: \\Histone deacetylase 6 structure and molecular basis of catalysis and inhibition\\ | 2016 | Nature chemical biology, 09, Volume: 12, Issue:9 | Histone deacetylase 6 structure and molecular basis of catalysis and inhibition. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 58 (8.61) | 29.6817 |
| 2010's | 477 (70.77) | 24.3611 |
| 2020's | 139 (20.62) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.
| This Compound (48.38) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 95 (14.01%) | 5.53% |
| Reviews | 72 (10.62%) | 6.00% |
| Case Studies | 10 (1.47%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 501 (73.89%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Phase I Study of the Combination of Bevacizumab, Everolimus and LBH589 (BEL) for the Treatment of Advanced Solid Tumors [NCT01055795] | Phase 1 | 14 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| A Phase Ib, Open-label, Multi-center Dose-finding Study of Oral Panobinostat (LBH589) in Combination With Ara-C and Mitoxantrone as Salvage Therapy for Refractory or Relapsed Acute Myeloid Leukemia [NCT01055483] | Phase 1 | 59 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| A Phase IB Study of the Histone Deacetylase Inhibitor Panobinostat (LBH589) Given Orally in Combination With Carboplatin and Paclitaxel in Patients With Advanced Solid Tumors [NCT01159418] | Phase 1 | 36 participants (Anticipated) | Interventional | 2008-06-30 | Active, not recruiting | ||
| A Pilot/Phase I Study of Panobinostat (LBH589) in Patients With Metastatic Melanoma [NCT01065467] | Phase 1 | 16 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
| A Phase I Dose Finding Study Of Panobinostat In Children With Refractory Hematologic Malignancies [NCT01321346] | Phase 1 | 30 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| A Phase Ib, Dose-finding Study of Oral Panobinostat (LBH589) in Combination With Idarubicin and Cytarabine Induction and High-dose Cytarabine-based Consolidation Therapy in Adult Patients Less Than or Equal to 65 Years Old With Acute Myeloid Leukemia (AML [NCT01242774] | Phase 1 | 46 participants (Actual) | Interventional | 2010-10-31 | Completed | ||
| A Phase I/II Open Label Study of LBH589, a Novel Histone Deacetylase Inhibitor (HDACi), in Patients With Primary Myelofibrosis (PMF) and Post-polycythemia/Essential Thrombocythemia Myelofibrosis (Post-PV/ET MF) [NCT01298934] | Phase 1/Phase 2 | 22 participants (Actual) | Interventional | 2009-09-30 | Active, not recruiting | ||
| A Phase 1 Study of HDAC Inhibitor Panobinostat (LBH 589) Administered in Combination With Ipilimumab in Subjects With Unresectable Stage III or Stage IV Melanoma [NCT02032810] | Phase 1 | 17 participants (Actual) | Interventional | 2014-01-07 | Completed | ||
| Efficacy and Safety Assessment of Oral LBH589 in Adult Patients With Advanced Soft Tissue Sarcoma After Pre-treatment Failure: an Open-label, Multicenter Phase II Study [NCT01136499] | Phase 2 | 53 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Phase Ib Study to Assess Safety and Tolerability of PDR001 in Combination With Panobinostat in Metastatic Melanoma and Non-small Cell Lung Cancer After Failure of Prior Anti PD1 or PD-L1 Therapy [NCT03982134] | Phase 1 | 0 participants (Actual) | Interventional | 2019-09-30 | Withdrawn(stopped due to Sponsor decision to withdraw) | ||
| Multicenter Phase I Study of Imatinib, a Platelet-derived Growth Factor Receptor Inhibitor, and LBH589, a Histone Deacetylase Inhibitor, in the Treatment of Newly Diagnosed and Recurrent Chordoma [NCT01175109] | Phase 1 | 36 participants (Anticipated) | Interventional | 2011-10-31 | Active, not recruiting | ||
| Evaluation of Panobinostat (LBH589) as Maintenance Therapy in Multiple Myeloma Following Autologous Hematopoietic Cell Transplantation [NCT02722941] | Phase 2 | 30 participants (Actual) | Interventional | 2016-06-10 | Completed | ||
| Phase I/II Study of the Combination of Panobinostat and Carfilzomib in Patients With Relapsed/Refractory Multiple Myeloma [NCT01496118] | Phase 1/Phase 2 | 80 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
| A Phase II, Multicentre Study of Oral LBH589 in Patients With Chronic Phase Chronic Myeloid Leukemia With Resistant Disease Following Treatment With at Least Two Fusion Gene of the BCR and ABL Genes (BCR-ABL) Tyrosine Kinase Inhibitors [NCT00451035] | Phase 2 | 29 participants (Actual) | Interventional | 2007-02-19 | Terminated | ||
| CLBH589DUS108T: Panobinostat With Carfilzomib and Dexamethasone for Relapsed/Refractory Multiple Myeloma: Correlation With In Vitro Chemosensitivity Testing [NCT03256045] | Phase 2 | 9 participants (Actual) | Interventional | 2018-02-08 | Terminated(stopped due to Terminated due to loss of funding and former PI left the institution) | ||
| A Phase 2 Study of Panobinostat in Combination With Everolimus for Children and Young Adults With Gliomas Harboring H3.3 or H3.1 K27M Mutation [NCT03632317] | Phase 2 | 0 participants (Actual) | Interventional | 2019-10-31 | Withdrawn(stopped due to low accrual) | ||
| A Phase I/II Multicenter, National, Open-Label Study of Panobinostat in Combination With Idarubicin and Cytarabine in Patients Aged 65 Years or Older With Newly Diagnosed Acute Myeloblastic Leukaemia (AML) [NCT00840346] | Phase 1/Phase 2 | 46 participants (Anticipated) | Interventional | 2009-09-30 | Completed | ||
| An Expanded Treatment Protocol of Panobinostat (LBH589) in Combination With Bortezomib and Dexamethasone in Patients With Multiple Myeloma Who Have Had at Least One Prior Line of Therapy [NCT02204553] | 0 participants | Expanded Access | No longer available | ||||
| A Randomized Phase II Study of Oral Panobinostat (LBH589) With or Without Rituximab to Treat Relapsed or Refractory Diffuse Large B Cell Lymphoma [NCT01238692] | Phase 2 | 42 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
| A Randomized, Phase II Trial Evaluating the Efficacy and Safety of Lenalidomide, Bortezomib and Dexamethasone (RVD) With or Without Panobinostat in Transplant Eligible, Newly Diagnosed Multiple Myeloma [NCT02720510] | Phase 2 | 6 participants (Actual) | Interventional | 2016-06-14 | Terminated(stopped due to A study was terminated due to low enrollment.) | ||
| A Phase II, Multi-center, Single Arm, Open Label Study to Evaluate the Efficacy and Safety of Panobinostat in Combination With Bortezomib and Dexamethasone in Japanese Patients With Relapsed/Refractory Multiple Myeloma [NCT02290431] | Phase 2 | 31 participants (Actual) | Interventional | 2014-12-16 | Completed | ||
| Phase II Study of Panobinostat (LBH589) for Recurrent Glioblastoma (GBM) Undergoing Planned Surgical Resection [NCT01115036] | Phase 2 | 0 participants (Actual) | Interventional | 2010-04-30 | Withdrawn(stopped due to No subjects were enrolled on this study, so study was closed and IND withdrawn.) | ||
| Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524] | Phase 1 | 2 participants (Actual) | Interventional | 2020-04-01 | Active, not recruiting | ||
| A Phase II Study of the Histone Deacetylase Inhibitor Panobinostat (LBH589) in Patients With Advanced Small Cell Lung Cancer (SCLC) [NCT01222936] | Phase 2 | 21 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| A Phase II Study of Oral LBH589 in Adult Patients With Refractory Cutaneous T-Cell Lymphoma [NCT00425555] | Phase 2 | 139 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
| A Disease Registry Encompassing the Care of Patients With Multiple Myeloma on Panobinostat (RECOMM) [NCT04150289] | 248 participants (Actual) | Observational [Patient Registry] | 2019-11-04 | Completed | |||
| Phase I Clinical Trial With LBH589 and Infusional 5-FU/LV in Patients With Metastatic Colorectal Cancer Who Failed 5-FU Based Chemotherapy [NCT01238965] | Phase 1 | 7 participants (Actual) | Interventional | 2010-10-31 | Terminated(stopped due to Adverse Events) | ||
| A Phase I Dose Finding Study of the Pan-DAC Inhibitor Panobinostat (LBH589) in Combination With Etoposide and Cisplatin in the First Line Treatment of Extensive-Stage Small Cell Lung Cancer - An ICORG In-House Study [NCT01160731] | Phase 1 | 0 participants (Actual) | Interventional | 2009-11-30 | Withdrawn | ||
| A Phase II Study of Panobinostat in Pediatric, Adolescent and Young Adult Patients With Solid Tumors Including Osteosarcoma, Malignant Rhabdoid Tumor/Atypical Teratoid Rhabdoid Tumors and Neuroblastoma [NCT04897880] | Phase 2 | 25 participants (Actual) | Interventional | 2019-01-09 | Terminated(stopped due to Drug supply) | ||
| Phase I Trial of Cisplatin and Pemetrexed in Combination With Panobinostat in Advanced Solid Tumors, With Emphasis on Non-Small Cell Lung Cancer [NCT01336842] | Phase 1 | 23 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| A Safety and Tolerability Study of RAD001 (mTOR Inhibitor) in Combination With Two Dosing Schedules of LBH589B (Histone Deacetylase Inhibitor) in Solid Tumors/ Lymphomas With Enrichment for EBV-Driven Tumors [NCT01341834] | Phase 1 | 49 participants (Actual) | Interventional | 2010-03-31 | Active, not recruiting | ||
| Panobinostat in Combination With Rituximab For Relapsed/Refractory Diffuse Large B Cell Lymphoma [NCT01282476] | Phase 2 | 18 participants (Actual) | Interventional | 2011-06-30 | Terminated(stopped due to slow accrual) | ||
| A One Year, Open Label, Multicenter Trial of LBH589 Alone or in Combination With ESA in Red Blood Cell Transfusion-dependent LOW and INT-1 MDS Patients Being Either Refractory to ESA or With a Low Probability of Response - the GErman PAnobinostat Low Risk [NCT01034657] | Phase 2 | 34 participants (Actual) | Interventional | 2009-11-30 | Terminated(stopped due to The study was terminated due to lack of efficacy of single agent LBH589 in the 4 month open label core phase and due to enrollment difficulties.) | ||
| A Phase II Trial of LBH589 in Patients With Metastatic Medullary Thyroid Cancer and Radioactive Iodine Resistant Differentiated Thyroid Cancer [NCT01013597] | Phase 2 | 13 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Phase 1 Trial of Panobinostat in Children With Diffuse Intrinsic Pontine Glioma [NCT02717455] | Phase 1 | 53 participants (Actual) | Interventional | 2016-06-28 | Active, not recruiting | ||
| Phase I Study of LBH589 in Combination With Erlotinib for Advanced Aerodigestive Tract Cancers (CLBH5889CUS11T) [NCT00738751] | Phase 1 | 44 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
| An Open-label, Multi-center, Expanded Treatment Protocol of Oral Panobinostat in Combination With Bortezomib and Dexamethasone in Patients With Relapsed, and Relapsed and Refractory Multiple Myeloma [NCT02568943] | 0 participants | Expanded Access | No longer available | ||||
| A Phase I/IIa Trial of VTD-panobinostat Treatment and Panobinostat Maintenance in Relapsed and Relapsed/Refractory Multiple Myeloma Patients [NCT02145715] | Phase 1/Phase 2 | 54 participants (Anticipated) | Interventional | 2013-01-31 | Active, not recruiting | ||
| Panobinostat and Ruxolitinib In MyElofibrosis (PRIME STUDY) - Phase I/II Study of Combination Oral JAK2 Tyrosine Kinase Inhibitor (JAK2-TKI) and Histone Deacetylase Inhibitor (HDACI) Therapy in Patients With Myelofibrosis [NCT01693601] | Phase 1/Phase 2 | 15 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
| Phase I Study of LBH589, A Novel Oral Deacetylase Inhibitor in Patients With Recurrent or Refractory Hodgkin or Non-Hodgkin's Lymphoma [NCT01032148] | Phase 1 | 8 participants (Actual) | Interventional | 2009-12-31 | Terminated(stopped due to lack of funding) | ||
| Phase I/ II Trial of Carboplatin and Etoposide Plus LBH589 for Previously Untreated Extensive Stage Small Cell Lung Cancer [NCT00958022] | Phase 1 | 7 participants (Actual) | Interventional | 2009-09-30 | Terminated(stopped due to Based on the tolerabilty challenges of the combination) | ||
| A Phase II Study of Panobinostat (LBH589) as Second-Line Therapy in Patients With Chronic Graft-Versus-Host Disease [NCT01028313] | Phase 2 | 0 participants (Actual) | Interventional | Withdrawn(stopped due to A decision was made to not move forward with the study. No participants were enrolled or treated.) | |||
| Pilot Study Evaluating the Expression of ERB-B4 After Treatment With HDAC Inhibitor in ER+ Tamoxifen Refractory Breast Cancer [NCT00993642] | Early Phase 1 | 0 participants (Actual) | Interventional | 2009-09-30 | Withdrawn(stopped due to Lack of accrual) | ||
| An Open-label Phase 2 Study of Intravenous Bortezomib and Oral Panobinostat (LBH589) in Adult Patients With Relapsed/Refractory Peripheral T-cell Lymphoma or NK/T-cell Lymphoma After Failure of Conventional Chemotherapy [NCT00901147] | Phase 2 | 25 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Phase II Trial of LBH589 (Panobinostat) in Relapsed or Relapsed and Refractory Waldenstrom's Macroglobulinemia [NCT00936611] | Phase 2 | 39 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| A Phase II Study of Oral Single Agent Panobinostat in Patients With Refractory de Novo or Secondary Acute Myelogenous Leukemia (AML) [NCT00880269] | Phase 2 | 59 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
| A Randomized, Triple-arm, Controlled, Open-label, Multicenter Phase II Study Assessing Two Different Doses of Panobinostat in Combination With Carfilzomib and Dexamethasone in Relapsed or Relapsed and Refractory Multiple Myeloma [NCT02756663] | Phase 2 | 0 participants (Actual) | Interventional | 2016-12-31 | Withdrawn | ||
| A Multicenter, Randomized, Open-label Phase 2 Study Evaluating the Safety and Efficacy of Three Different Regimens of Oral Panobinostat in Combination With Subcutaneous Bortezomib and Oral Dexamethasone in Patients With Relapsed or Relapsed/Refractory Mul [NCT02654990] | Phase 2 | 249 participants (Actual) | Interventional | 2016-04-27 | Completed | ||
| Open Label, Multi-center, Phase IV Study of Ruxolitinib or Ruxolitinib and Panobinostat Combination, for Patients Who Have Completed Prior Global Novartis or Incyte Sponsored Studies [NCT02386800] | Phase 4 | 356 participants (Anticipated) | Interventional | 2015-03-05 | Recruiting | ||
| A Phase II Study of Oral LBH589 in Adult Patients With Cutaneous T-Cell Lymphoma Who Are Intolerant to or Have Progressed on or After Prior HDAC Inhibitor [NCT00490776] | Phase 2 | 9 participants (Actual) | Interventional | 2007-07-05 | Terminated(stopped due to Recruitment was stopped on 15 June 2009 (early termination date) due to low prevalence of study population and slow accrual.) | ||
| A Phase I Study Evaluating the Combination of the Deacetylase Inhibitor, LBH589 Plus the mTOR Inhibitor RAD001, in Relapsed and Refractory Adult Patients With Lymphoma [NCT00962507] | Phase 1 | 11 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| Phase I, Dose Finding Trial of the Combination of Panobinostat and Stereotactic Radiation in the Treatment of Brain Tumors [NCT01324635] | Phase 1 | 17 participants (Actual) | Interventional | 2012-05-31 | Terminated(stopped due to Arm A - reached goal; Arm B - poor accrual) | ||
| A Phase II Study Of Oral LBH589 In Adult Patients With Multiple Myeloma Who Have Received At Least Two Prior Lines Of Therapy And Whose Disease Is Refractory To The Most Recent Line Of Therapy [NCT00445068] | Phase 2 | 38 participants (Actual) | Interventional | 2007-04-16 | Terminated | ||
| A Phase II Study of Oral LBH589 in Patients With Cutaneous T-cell Lymphoma and Adult T-cell Leukemia/Lymphoma [NCT00699296] | Phase 2 | 4 participants (Actual) | Interventional | 2008-05-31 | Terminated | ||
| A Phase I and Dose Expansion Cohort Study of Panobinostat in Combination With Fludarabine and Cytarabine in Pediatric Patients With Refractory or Relapsed Acute Myeloid Leukemia or Myelodysplastic Syndrome [NCT02676323] | Phase 1 | 19 participants (Actual) | Interventional | 2016-05-03 | Terminated(stopped due to Slow accrual) | ||
| A Phase I Study of LBH589 (Panobinostat) in Combination With External Beam Radiotherapy for the Treatment of Prostate Cancer, Esophageal Cancer and Head and Neck Cancer [NCT00670553] | Phase 1 | 7 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
| Phase II Trial of LBH589 in Refractory Colorectal Cancer [NCT00690677] | Phase 2 | 29 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| A Phase I/II Study of Oral Melphalan Combined With LBH589 for Patients With Relapsed or Refractory Multiple Myeloma (MM) [NCT00743288] | Phase 1/Phase 2 | 40 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| A Phase II, Multicentre Study of Oral LBH589 in Patients With Accelerated Phase or Blast Phase (Blast Crisis) Chronic Myeloid Leukemia With Resistant Disease Following Treatment With at Least Two BCR-ABL Tyrosine Kinase Inhibitors [NCT00449761] | Phase 2 | 27 participants (Actual) | Interventional | 2007-02-23 | Terminated | ||
| A Phase Ib, Open-label, Two Arm Study of i.v. and Oral Panobinostat (LBH589) in Combination With i.v. Trastuzumab (Herceptin®) and i.v. Paclitaxel as Treatment for Adult Female Patients With HER2 Overexpressing Metastatic Breast Cancer (MBC) [NCT00788931] | Phase 1 | 15 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
| Phase Ib/II: Epigenetic Modification of Chemosensitivity and Apoptosis in Metastatic Melanoma: Treatment of a Resistant Disease Using Decitabine, Temozolomide and Panobinostat [NCT00925132] | Phase 1/Phase 2 | 39 participants (Actual) | Interventional | 2009-12-31 | Terminated(stopped due to Change in the number of approved drugs for metastatic melanoma) | ||
| A Phase IA/II, Two-arm, Multi-center, Open-label, Dose-escalation Study of LBH589 Administered Orally Via Different Dosing Schedules in Adult Patients With Advanced Hematological Malignancies [NCT00621244] | Phase 1/Phase 2 | 175 participants (Actual) | Interventional | 2003-03-01 | Completed | ||
| A Phase Ib/IIb, Open-label, Multi-center, Study of Oral Panobinostat (LBH589) Administered With 5-Azacitidine (in Adult Patients With Myelodysplastic Syndromes (MDS), Chronic Myelomonocytic Leukemia (CMML), or Acute Myeloid Leukemia (AML). [NCT00946647] | Phase 1/Phase 2 | 113 participants (Actual) | Interventional | 2009-12-02 | Completed | ||
| A Phase I/II Study of LBH589 Plus Decitabine for Patients Age ≥ 60 Years With High Risk MDS or AML [NCT00691938] | Phase 1/Phase 2 | 52 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
| Phase II Trial of LBH589 (Panobinostat) in Adult Patients With Recurrent Malignant Gliomas [NCT00848523] | Phase 2 | 6 participants (Actual) | Interventional | 2008-11-30 | Terminated(stopped due to insufficient accrual) | ||
| A Phase I/II Study of the Histone Deacetylase (HDAC) Inhibitor LBH589 (Panobinostat) in Combination With mTOR Inhibitor RAD001 (Everolimus) in Patients With Relapsed Multiple Myeloma or Lymphoma [NCT00918333] | Phase 1/Phase 2 | 124 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| Phase II Trial of Oral LBH 589, a Novel Histone Deacetylase (HDAC) Inhibitor, in Relapsed or Refractory Chronic Lymphocytic Leukemia and Mantle Cell Lymphoma [NCT01090973] | Phase 2 | 1 participants (Actual) | Interventional | 2010-03-31 | Terminated(stopped due to Pharmaceutical company request.) | ||
| Phase I Exploratory Study of Panobinostat IV in Combination With Bortezomib in Relapsed/Refractory Multiple Myeloma Patients [NCT00891033] | Phase 1 | 12 participants (Actual) | Interventional | 2009-04-30 | Terminated(stopped due to This study was terminated because the drug company stopped making the study drug) | ||
| Pemetrexed and LBH589 in Previously-Treated Patients With Advanced Non-Small Cell Lung Cancer [NCT00907179] | Phase 1 | 12 participants (Actual) | Interventional | 2009-07-31 | Terminated(stopped due to Widespread use firstline Pemetrexed; slow recruitment; funding withdrawn..) | ||
| A Phase I Dose Escalation Study of LBH589 in Combination With Imatinib Mesylate for Patients With Chronic Myeloid Leukemia in Cytogenetic Remission With Residual Disease Detectable by Q-PCR [NCT00686218] | Phase 1 | 9 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| Phase I/II Study of LBH589 and Bevacizumab in Patients With Recurrent High Grade Glioma [NCT00859222] | Phase 1/Phase 2 | 51 participants (Actual) | Interventional | 2009-03-31 | Completed | ||
| A Phase Ib/IIa Trial of Panobinostat in Combination With Trastuzumab in Adult Female Patients With HER2 Positive Metastatic Breast Cancer Whose Disease Has Progressed During or Following Therapy With Trastuzumab [NCT00567879] | Phase 1/Phase 2 | 56 participants (Actual) | Interventional | 2008-04-30 | Terminated(stopped due to The study was terminated early due to insufficient evidence of clinical benefit.) | ||
| A Phase II, Open-label Multicenter Trial of Panobinostat Monotherapy in Women With HER2-negative Locally Recurrent or Metastatic Breast Cancer [NCT00777049] | Phase 2 | 54 participants (Actual) | Interventional | 2009-02-28 | Completed | ||
| A Phase II, Open Label, Single Arm Study of i.v. Panobinostat (LBH589) in Patients With Metastatic Hormone Refractory Prostate Cancer [NCT00667862] | Phase 2 | 35 participants (Actual) | Interventional | 2008-03-18 | Completed | ||
| A Phase II Study of Oral Panobinostat in Adult Patients With Relapsed/Refractory Classical Hodgkins Lymphoma After High-dose Chemotherapy With Autologous Stem Cell Transplant [NCT00742027] | Phase 2 | 129 participants (Actual) | Interventional | 2008-09-16 | Completed | ||
| A Phase I, Open-label, Multicenter Study to Evaluate the Pharmacokinetics and Safety of Oral Panobinostat in Patients With Advanced Solid Tumors and Various Degrees of Hepatic Function [NCT01007968] | Phase 1 | 25 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| A Phase I Trial of Sorafenib and LBH589 in the Treatment of Advanced HCC [NCT00823290] | Phase 1 | 2 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to Investigator left site) | ||
| Phase I/II Randomized Trial of LBH589 (Panobinostat) at Two Dose Levels Combined With Bicalutamide (Casodex) in Men With Castration-resistant Prostate Cancer [NCT00878436] | Phase 1/Phase 2 | 52 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| A Phase I Trial of Panobinostat (LBH589) and Epirubicin in Patients With Solid Tumor Malignancies [NCT00878904] | Phase 1 | 40 participants (Actual) | Interventional | 2009-09-13 | Completed | ||
| A Phase Ib, Multi-center, Open-label, Dose-escalation Study of Oral LBH589 When Administered in Combination With Oral Lenalidomide & Dexamethasone in Adult Patients With Multiple Myeloma [NCT00532675] | Phase 1 | 46 participants (Actual) | Interventional | 2008-04-22 | Completed | ||
| A Phase II Study of LBH589, a Novel Histone Deacetylase Inhibitor, in Relapsed and Refractory Adult Patients With Acute Leukemia (AL) or in Newly Diagnosed Patients Over the Age of 60 [NCT00723203] | Phase 2 | 16 participants (Actual) | Interventional | 2008-04-30 | Terminated(stopped due to Terminated early due to a lack of efficacy) | ||
| A Phase IB, Open-Label, Multicenter Study to Investigate the Effect of Oral LBH589 on Dextromethorphan, a CYP2D6 Substrate, and to Assess the Efficacy and Safety of Oral LBH589 in Patients With Advanced Solid Tumors [NCT00535951] | Phase 1 | 18 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| A Phase I Safety and Tolerability Study of LBH589 in Combination With Sorafenib in Patients With Advanced Renal Cell Carcinoma, Soft Tissue Sarcoma, and Non-small Cell Lung Carcinoma (NSCLC) of Non-squamous Histologies. [NCT01005797] | Phase 1 | 38 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| Panobinostat Combined With High-Dose Gemcitabine/Busulfan/Melphalan With Autologous Stem Cell Transplant for Patients With Refractory/Relapsed Myeloma [NCT02506959] | Phase 2 | 83 participants (Actual) | Interventional | 2015-09-14 | Active, not recruiting | ||
| Phase I, Prospective, Open-label, Multi-centric, Dose Finding Trial of Combination of IGEV and Panobinostat Before Autologous Stem Cell Transplant in Patients With Hodgkin's Lymphoma [NCT01884428] | Phase 1 | 24 participants (Anticipated) | Interventional | 2011-07-31 | Recruiting | ||
| Panobinostat Combined With High-Dose Gemcitabine/Busulfan/Melphalan With Autologous Stem Cell Transplant for Patients With Refractory/Relapsed Lymphoma [NCT02961816] | Phase 2 | 0 participants (Actual) | Interventional | 2017-06-30 | Withdrawn(stopped due to Lack of funding) | ||
| A Phase I Open Label Study Of Panobinostat In Combination With Lenalidomide, Bortezomib, And Dexamethasone In Patients With Relapsed And Relapsed/Refractory Multiple Myeloma [NCT01965353] | Phase 1 | 21 participants (Actual) | Interventional | 2013-10-31 | Completed | ||
| A Phase I Dose-escalation Study of LBH589 Administered Orally in Adult Patients With Advanced Solid Tumors or Cutaneous T-cell Lymphoma [NCT00412997] | Phase 1 | 14 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
| Phase I/II Trial of Tamoxifen Following Epigenetic Regeneration of Estrogen Receptor Using Decitabine and LBH 589 in Patients With Triple Negative Metastatic Breast Cancer [NCT01194908] | Phase 1/Phase 2 | 5 participants (Actual) | Interventional | 2010-07-31 | Terminated(stopped due to Slow accrual) | ||
| Phase Ib, Open-label, Multi-center Study to Characterize the Safety, Tolerability and Pharmacodynamics (PD) of PDR001 in Combination With LCL161, Everolimus (RAD001) or Panobinostat (LBH589) [NCT02890069] | Phase 1 | 298 participants (Actual) | Interventional | 2016-10-14 | Completed | ||
| A Phase Ib Open-label, Multicenter Cross-over Study to Investigate the Effect of Food on the Rate and Extent of Oral LBH589 Absorption in Patients With Advanced Solid Tumors [NCT00570284] | Phase 1 | 36 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
| A Phase II, Multi-center, Single Arm, Open Label Study of Panobinostat in Combination With Bortezomib and Dexamethasone in Patients With Relapsed and Bortezomib-refractory Multiple Myeloma [NCT01083602] | Phase 2 | 55 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| A Phase I Study of LBH589 in Combination With Paclitaxel and Carboplatin +/- Bevacizumab the Treatment of Solid Tumors [NCT00556088] | Phase 1 | 40 participants (Anticipated) | Interventional | 2007-12-31 | Completed | ||
| A Phase I, Open-label, Multi-center Study to Evaluate the Pharmacokinetics and Safety of Oral Panobinostat in Patients With Advanced Solid Tumors and Varying Degrees of Renal Function [NCT00997399] | Phase 1 | 37 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| A Phase IA, Dose-escalating Study of LBH589 Administered Intravenously in Adult Patients With Advanced Solid Tumors [NCT00739414] | Phase 1 | 14 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
| A Phase III Randomized, Double Blind, Placebo Controlled Multi-center Study of Panobinostat for Maintenance of Response in Patients With Hodgkin's Lymphoma Who Are at Risk for Relapse After High Dose Chemotherapy and Autologous Stem Cell Transplant (ASCT) [NCT01034163] | Phase 3 | 41 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| Phase II Trial of Oral Panobinostat (LBH589), a Novel Deacetylase Inhibitor (DACi) in Patients With Primary Myelofibrosis (PMF), Post Essential Thrombocythemia (ET) Myelofibrosis and Post- Polycythemia Vera (PV) Myelofibrosis [NCT00931762] | Phase 2 | 35 participants (Actual) | Interventional | 2009-08-31 | Terminated | ||
| Phase I Study of Panobinostat Plus ICE Chemotherapy Followed by a Randomized Phase-II Study of ICE Compared With Panobinostat Plus ICE for Patients With Relapsed and Refractory Classical Hodgkin Lymphoma [NCT01169636] | Phase 1/Phase 2 | 62 participants (Actual) | Interventional | 2011-01-31 | Completed | ||
| A Phase 2 Study to Evaluate the Efficacy of Epigenetic Modulation in Relapsed/Refractory Diffuse Large B-Cell Lymphoma (DLBCL) [NCT00978432] | Phase 2 | 50 participants (Actual) | Interventional | 2012-02-29 | Terminated(stopped due to The toxicity seemed to outweigh the benefit.) | ||
| An Open Label, Single Arm, Phase Ib Dose Finding Study of i.v. Panobinostat (LBH589) With Docetaxel and Prednisone in Patients With Hormone Refractory Prostate Cancer [NCT00663832] | Phase 1 | 44 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
| A Phase I/II Trial Evaluating the Use of Histone Deacetylase Inhibitor LBH589 in Addition to Corticosteroids in Patients With Acute Graft Versus Host Disease [NCT01111526] | Phase 1/Phase 2 | 22 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
| Phase I-II Study of Carfilzomib, Lenalidomide, Dexamethasone, and Panobinostat, Ca-R-Pa-Diem, as Induction Therapy for Newly Diagnosed, Untreated, Transplant-Eligible, Multiple Myeloma Patients [NCT02802163] | Phase 1/Phase 2 | 0 participants (Actual) | Interventional | 2017-06-30 | Withdrawn(stopped due to study drug unavailable) | ||
| A Phase I Study of LBH589 in Combination With Gemcitabine in the Treatment of Solid Tumors [NCT00550199] | Phase 1 | 17 participants (Actual) | Interventional | 2007-11-30 | Terminated(stopped due to Study terminated due to LBH589 toxicity.) | ||
| Phase I Study of Combination of Sorafenib and LBH589 in Hepatocellular Carcinoma [NCT00873002] | Phase 1 | 3 participants (Actual) | Interventional | 2009-03-31 | Terminated(stopped due to Dose Limiting Toxicity) | ||
| A Phase I Study of Panobinostat in Combination With Daratumumab, Bortezomib, and Dexamethasone in Patients With Relapsed/Refractory Multiple Myeloma [NCT04956302] | Phase 1 | 1 participants (Actual) | Interventional | 2021-09-27 | Terminated(stopped due to PI Decision) | ||
| A Multicenter, Randomized, Double Blind, Placebo Controlled Phase III Study of Panobinostat in Combination With Bortezomib and Dexamethasone in Patients With Relapsed Multiple Myeloma [NCT01023308] | Phase 3 | 767 participants (Actual) | Interventional | 2009-12-21 | Completed | ||
| Phase 1 Trial of Marizomib Alone and in Combination With Panobinostat for Children With Diffuse Intrinsic Pontine Glioma [NCT04341311] | Phase 1 | 45 participants (Anticipated) | Interventional | 2020-08-10 | Active, not recruiting | ||
| An Open-label, Single Center, Study to Determine the Absorption, Distribution, Metabolism, and Excretion (ADME) of LBH589 After a Single Oral Administration of 20 mg (14C) LBH589 in Advanced Cancer Patients [NCT00472368] | Phase 1 | 4 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
| A Phase IB, Study to Investigate the Effect of Ketoconazole, a CYP3A4 Inhibitor, on Oral LBH589 and to Assess the Efficacy and Safety of Oral LBH589 in Patients With Advanced Solid Tumors. [NCT00503451] | Phase 1 | 14 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
| A Phase IA/IB, Two Arm, Multi-center, Open-label, Dose Escalation Study of Oral LBH589 Alone and in Combination With IV Docetaxel and Oral Prednisone in Hormone Refractory Prostate Cancer (HRPC) [NCT00493766] | Phase 1 | 16 participants (Actual) | Interventional | 2006-05-31 | Terminated(stopped due to Because of a strategic decision by Novartis) | ||
| A Phase Ib, Multi-center, Open-label, Dose-escalation Study of Oral LBH589 When Administered in Combination With Bortezomib in Adult Patients With Multiple Myeloma [NCT00532389] | Phase 1 | 62 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
| Phase II Study of LBH589 for Patients With Low or Intermediate-1 Risk Myelodysplastic Syndrome [NCT00939159] | Phase 2 | 17 participants (Actual) | Interventional | 2009-08-31 | Terminated(stopped due to Low Accrual) | ||
| A Phase IA/IB, Two Arm, Multi-center, Open-label, Dose Escalation Study of Oral LBH589 Alone and in Combination With IV Docetaxel and Oral Prednisone in Hormone Refractory Prostate Cancer (HRPC) [NCT00419536] | Phase 1 | 108 participants | Interventional | 2006-05-31 | Terminated | ||
| Phase I/II of Panobinostat (LBH589) Plus Everolimus (RAD001) in Patients With Relapsed and Refractory Lymphoma [NCT00967044] | Phase 1/Phase 2 | 31 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
| A Phase II Trial of Panobinostat and Lenalidomide in Patients With Relapsed or Refractory Hodgkin's Lymphoma [NCT01460940] | Phase 2 | 24 participants (Actual) | Interventional | 2011-10-13 | Completed | ||
| An Open-label, Uncontrolled Phase II Trial of HDAC-Inhibitor LBH589 in Patients With Chemo-refractory Metastatic Gastric Cancer Overexpressing Histone Deacetylases (HDACs) - CLBH589BDE03T [NCT01528501] | Phase 2 | 28 participants (Anticipated) | Interventional | 2009-06-30 | Terminated(stopped due to medical/ethical reasons) | ||
| A Phase I Study of the Combination of Panobinostat and Carfilzomib in Patients With Relapsed and/or Refractory Multiple Myeloma [NCT01549431] | Phase 1 | 32 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| A Phase I-II Pilot Study to Assess the Safety and Efficacy of Combined Administration With Pegylated Interferon-alpha2a and the Histone Deacetylase Inhibitor (HDACi) Panobinostat for Reducing the Residual Reservoir of HIV-1 Infected Cells in cART-Treated [NCT02471430] | Phase 1/Phase 2 | 34 participants (Anticipated) | Interventional | 2016-05-31 | Active, not recruiting | ||
| A Phase II Study of LBH589 in the Treatment of Patients With Refractory Clear Cell Renal Carcinoma [NCT00550277] | Phase 2 | 20 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
| A Phase I Study of LBH589 in Combination With Capecitabine ± Lapatinib [NCT00632489] | Phase 1 | 20 participants (Actual) | Interventional | 2008-05-31 | Completed | ||
| A Randomized Phase II, Open-label Multicenter Trial of Panobinostat Monotherapy in Women With HER2 Positive Locally Recurrent or Metastatic Breast Cancer [NCT00777335] | Phase 2 | 4 participants (Actual) | Interventional | 2009-02-28 | Terminated(stopped due to Very low recruitement rate.) | ||
| Study to Investigate Outcome of Individualized Treatment Based on Pharmacogenomic Profiling & Ex Vivo Drug Sensitivity Testing of Patient-derived Organoids in Patients With Metastatic Colorectal Cancer [NCT05725200] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
| A Phase I/II Study of MLN9708 (Ixazomib) in Combination With Panobinostat and Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma [NCT02057640] | Phase 1/Phase 2 | 16 participants (Actual) | Interventional | 2014-05-22 | Completed | ||
| A Phase I Study of Panobinostat in Combination With Bortezomib in the Treatment of Relapsed and/or Refractory Mantle Cell Lymphoma [NCT01504776] | Phase 1 | 3 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
| Phase I Study to Determine the Safety and Tolerability of Escalating Doses of Panobinostat (LBH589) in Patients With Sickle Cell Disease [NCT01245179] | Phase 1 | 18 participants (Anticipated) | Interventional | 2010-11-30 | Recruiting | ||
| The Safety and Efficacy of The Histone Deacetylase Inhibitor Panobinostat for Purging HIV-1 From The Latent Reservoir (CLEAR) Study [NCT01680094] | Phase 1/Phase 2 | 15 participants (Actual) | Interventional | 2012-09-30 | Completed | ||
| A Phase II Trial of LBH589 in Refractory Myelodysplastic Syndromes (MDS) Patients [NCT00594230] | Phase 2 | 26 participants (Actual) | Interventional | 2008-01-31 | Terminated(stopped due to Per protocol, the results of a planned interim analysis demonstrated insufficient efficacy and led to early termination of the study.) | ||
| A Phase II Study of Oral Panobinostat in Adult Patients With Diffuse Large B-cell Lymphoma Relapsed/Refractory After High-dose Chemotherapy With Autologous Stem Cell Transfusion (ASCT) or Not Eligible for ASCT [NCT01523834] | Phase 2 | 35 participants (Actual) | Interventional | 2011-02-28 | Completed | ||
| A Phase 1b, Open-label, Multi-center, Single Arm, Dose Finding Study to Assess Safety and Pharmacokinetics of the Oral Combination of Panobinostat and Ruxolitinib in Patients With Primary Myelofibrosis (PMF), Post-polycythemia Vera-myelofibrosis (PPV-MF) [NCT01433445] | Phase 1 | 61 participants (Actual) | Interventional | 2011-11-01 | Completed | ||
| Phase I/Ib Trial of the Efficacy and Safety of Combination Therapy of Lenalidomide/Bortezomib/Dexamethasone and Panobinostat in Transplant Eligible Patients With Newly Diagnosed Multiple Myeloma (MM) [NCT01440582] | Phase 1 | 77 participants (Actual) | Interventional | 2013-02-18 | Completed | ||
| A Phase I Dose Finding and Proof-of-concept Study of the Histone Deacetylase Inhibitor Panobinostat (LBH589) in Combination With Standard Dose Cytarabine and Daunorubicin for Older Patients With Untreated Acute Myeloid Leukemia or Advanced Myelodysplastic [NCT01463046] | Phase 1 | 29 participants (Actual) | Interventional | 2012-01-31 | Completed | ||
| Phase II Study of Panobinostat (LBH589) Given in Combination With Bortezomib (Velcade) in Patients With Pancreatic Cancer Progressing on Gemcitabine Therapy Alone or Gemcitabine in Combination [NCT01056601] | Phase 2 | 7 participants (Actual) | Interventional | 2010-09-30 | Terminated(stopped due to Funding not available) | ||
| A Phase II Trial of Panobinostat in Patients With Neuroendocrine Tumors [NCT00985946] | Phase 2 | 15 participants (Actual) | Interventional | 2010-05-31 | Terminated(stopped due to Study did not meet statistical requirements to continue.) | ||
| An Open Label Single Arm Phase I/II Study of MTX110 Delivered by Convection-enhanced Delivery (CED) in Patients With Diffuse Intrinsic Pontine Glioma (DIPG) Previously Treated With External Beam Radiation Therapy [NCT03566199] | Phase 1/Phase 2 | 7 participants (Actual) | Interventional | 2018-05-22 | Completed | ||
| A Phase II Study Incorporating Panobinostat, Bortezomib and Liposomal Vincristine Into Re-Induction Therapy for Relapsed Pediatric T-Cell Acute Lymphoblastic Leukemia or Lymphoma [NCT02518750] | Phase 2 | 3 participants (Actual) | Interventional | 2016-11-23 | Terminated(stopped due to Due to slow accrual) | ||
| A Phase II Trial Evaluating the Use of a Histone Deacetylase Inhibitor Panobinostat for Graft Versus Host Disease (GVHD) Prevention [NCT02588339] | Phase 2 | 42 participants (Actual) | Interventional | 2016-03-04 | Completed | ||
| A Phase Ib, Open-label, Multi-center, Dose-escalation Study of Oral Panobinostat (LBH589) Administered With 5-Azacitidine (Vidaza®) in Adult Japanese Patients With Myelodysplastic Syndromes (MDS), Chronic Myelomonocytic Leukemia (CMML) or Acute Myeloid Le [NCT01613976] | Phase 1 | 10 participants (Actual) | Interventional | 2012-08-31 | Completed | ||
| Phase I/II Study With Oral Panobinostat Maintenance Therapy Following Allogeneic Stem Cell Transplantation in Patients With High Risk MDS or AML (PANOBEST) [NCT01451268] | Phase 1/Phase 2 | 62 participants (Anticipated) | Interventional | 2011-01-31 | Active, not recruiting | ||
| Phase I/II Study of Panobinostat (LBH589) and Letrozole in Patients With Triple Negative Metastatic Breast Cancer [NCT01105312] | Phase 1/Phase 2 | 28 participants (Actual) | Interventional | 2010-09-30 | Completed | ||
| A Phase II Study to Investigate Biological Correlates of Clinical Response to Panobinostat in Haematological Malignancy [NCT01658241] | Phase 2 | 30 participants (Actual) | Interventional | 2012-07-16 | Completed | ||
| A Phase II, Single-Center, Open-Label Study Of Oral Panobinostat (LBH589) When Administered In Combination With Lenalidomide And Weekly Dexamethasone In Patients With Multiple Myeloma [NCT01651039] | Phase 2 | 32 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
| A Randomized, Multicenter Phase III Study to Assess the Efficacy of Panobinostat Maintenance Therapy vs. Standard of Care Following Allogeneic Stem Cell Transplantation in Patients With High-risk AML or MDS (ETAL-4 / HOVON-145) [NCT04326764] | Phase 3 | 52 participants (Actual) | Interventional | 2018-07-24 | Terminated(stopped due to Change of marketing authorisation holder) | ||
| A Phase I/II Study of the HDAC Inhibitor LBH-589 in Combination With the mTOR Inhibitor Everolimus (RAD001) in Metastatic Renal Cell Carcinoma [NCT01582009] | Phase 1/Phase 2 | 26 participants (Actual) | Interventional | 2010-03-31 | Terminated(stopped due to pts off study, PI left institute) | ||
| A Phase II Study of the Histone Deacetylase (HDAC) Inhibitor LBH589 (Panobinostat) in Patients With Relapsed or Refractory Non-Hodgkin Lymphoma [NCT01261247] | Phase 2 | 41 participants (Actual) | Interventional | 2011-01-17 | Completed | ||
| An Open-label Multi-center Single Agent Panobinostat Roll-over Protocol for Patients Who Have Completed a Previous Novartis-sponsored Panobinostat Study and Are Judged by the Investigator to Benefit From Continued Single Agent Panobinostat Treatment [NCT01802879] | Phase 2 | 9 participants (Actual) | Interventional | 2013-06-24 | Completed | ||
| A Feasibility Study Examining the Use of Non-Invasive Focused Ultrasound (FUS) With Oral Panobinostat Administration in Children With Progressive Diffuse Midline Glioma (DMG) [NCT04804709] | Phase 1 | 3 participants (Actual) | Interventional | 2021-07-28 | Active, not recruiting | ||
| Phase 1/1b Study of the Efficacy and Safety of the Combination of Panobinostat + Carfilzomib in Patients With Relapsed/Refractory Myeloma [NCT01301807] | Phase 1 | 63 participants (Actual) | Interventional | 2011-07-28 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||