methyl 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 400769 |
| CHEMBL ID | 1762621 |
| CHEBI ID | 177406 |
| SCHEMBL ID | 12521530 |
| MeSH ID | M0412359 |
| Synonym |
|---|
| HY-13324 |
| CSA:218600-53-4;BARDOXOLONE METHYL |
| nsc 713200; rta 402; cddo methyl ester |
| methyl (4as,6ar,6bs,8ar,12as,14ar,14bs)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylate |
| CHEBI:177406 |
| 218600-53-4 |
| nsc-713200 |
| cddo-me |
| nsc713200 |
| bardoxolone methyl , |
| bardoxolone-methyl |
| 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid methyl ester |
| cddo methyl ester |
| rta-402 |
| methyl 2-cyano-3,12-dioxoolean-1,9-dien-28-oate |
| methyl 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate |
| bardoxolone methyl ester |
| nsc 713200 |
| CHEMBL1762621 |
| rta 402 |
| cddo-methyl ester |
| NCGC00186460-01 |
| bardoxolone methyl (jan/usan) |
| D09585 |
| tox21_113229 |
| cas-218600-53-4 |
| dtxsid5048764 , |
| dtxcid2028690 |
| bardoxolone methyl [usan] |
| oleana-1,9(11)-dien-28-oic acid, 2-cyano-3,12-dioxo-, methyl ester |
| unii-ceg1q6ogu1 |
| ceg1q6ogu1 , |
| (+)-methyl 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oate |
| (4as,6ar,6bs,8ar,12as,14bs)-methyl 11-cyano-2,2,6a,6b,9,9,12a-he |
| CS-0598 |
| S8078 |
| 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid methyl ester |
| gtpl3443 |
| 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid methyl ester |
| bardoxolone methyl ester [mi] |
| bardoxolone methyl [jan] |
| rta402 |
| bardoxolone methyl [who-dd] |
| (4as,6ar,6bs,8ar,12as,14ar,14bs)-methyl 11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicene-4a-carboxylate |
| SCHEMBL12521530 |
| AC-26830 |
| AKOS025401880 |
| bardoxolone (methyl) |
| tp-155 |
| cddo methyl ester, >=98% (hplc) |
| bdbm217379 |
| cddo-me, 2 |
| BCP04660 |
| Q4860208 |
| DB05983 |
| WPTTVJLTNAWYAO-KPOXMGGZSA-N |
| CCG-269743 |
| A847580 |
| methyl (4as,6ar,6bs,12as,14ar,14br)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylate |
Bardoxolone methyl is an antioxidant modulator that acts through induction of the nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway. It has been shown to suppress various cancers and inflammation.
Bardoxolone methyl (CDDO-Me) has displayed promising anti-DN activity as well as serious side effects in clinical trials. The highly reactive α-cyano-α,β-unsaturated ketone (CUK) in ring A of CDDO- me can covalently bind to thiol functionalities in many biomacromolecules. Bardoxlone methyl has been reported to cause detrimental cardiovascular events in the terminated BEACON Phase III human clinical trial via modulation of the renal endothelin pathway.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Bardoxolone methyl (CDDO-Me) has displayed promising anti-DN activity as well as serious side effects in clinical trials, probably because the highly reactive α-cyano-α,β-unsaturated ketone (CUK) in ring A of CDDO-Me can covalently bind to thiol functionalities in many biomacromolecules." | ( Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. Chen, C; Huang, Z; Lai, Y; Li, P; Mou, Y; Peng, S; Tian, J; Xu, X; Xu, Y; Zhang, Y; Zhao, D, 2017) | 1.5 |
| "Bardoxolone methyl has been shown to increase eGFR in several clinical trials, including a phase 3 trial in patients with type 2 diabetes and stage 4 CKD (BEACON), which was terminated early due to an increase in heart failure events in bardoxolone methyl-treated patients. " | ( Effects of Bardoxolone Methyl on QT Interval in Healthy Volunteers. Chin, MP; Goldsberry, A; Meyer, CJ; O Apos Grady, M; Rich, S, 2019) | 2.35 |
| "Bardoxolone methyl has been reported to cause detrimental cardiovascular events in the terminated BEACON Phase III human clinical trial via modulation of the renal endothelin pathway. " | ( The endothelin pathway: a protective or detrimental target of bardoxolone methyl on cardiac function in patients with advanced chronic kidney disease? Camer, D; Huang, XF, 2014) | 2.09 |
| "Bardoxolone methyl (BARD) has been extensively studied for the treatment of chronic diseases." | ( Bardoxolone Methyl Prevents Fat Deposition and Inflammation in Brown Adipose Tissue and Enhances Sympathetic Activity in Mice Fed a High-Fat Diet. Camer, D; Dinh, CH; Huang, XF; Szabo, A; Wang, H; Yu, Y; Zhang, Q, 2015) | 2.58 |
Bardoxolone Methyl Evaluation in Patients with Chronic Kidney Disease and Type 2 Diabetes (BEACON) resulted in increases in estimated glomerular filtration rate (eGFR) with concurrent reductions in body weight.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with bardoxolone methyl in a multinational phase 3 trial, Bardoxolone Methyl Evaluation in Patients with Chronic Kidney Disease and Type 2 Diabetes (BEACON), resulted in increases in estimated glomerular filtration rate (eGFR) with concurrent reductions in body weight." | ( Effects of bardoxolone methyl on body weight, waist circumference and glycemic control in obese patients with type 2 diabetes mellitus and stage 4 chronic kidney disease. Appel, GB; Block, GA; Chertow, GM; Chin, MP; Coyne, DW; Goldsberry, A; Kalantar-Zadeh, K; Meyer, CJ; Molitch, ME; Pergola, PE; Raskin, P; Rossing, P; Silva, AL; Spinowitz, B; Sprague, SM, 2018) | 1.21 |
| "Treatment with bardoxolone methyl (Bard) in a multinational phase 3 trial, Bardoxolone Methyl Evaluation in Patients with Chronic Kidney Disease and Type 2 Diabetes (BEACON), resulted in increases in estimated glomerular filtration rate with concurrent reductions in serum magnesium. " | ( Effects of Bardoxolone Methyl on Magnesium in Patients with Type 2 Diabetes Mellitus and Chronic Kidney Disease. Chin, MP; Goldsberry, A; McCullough, PA; Meyer, CJ; O'Grady, M; Pergola, PE; Rizk, DV; Silva, AL; Toto, R; Warnock, DG, 2019) | 1.26 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In a Phase I trial in cancer patients, CDDO-Me was found to have a slow and saturable oral absorption, a relatively long terminal phase half-life (39 hours at 900 mg/day), nonlinearity (dose-dependent) at high doses (600-1,300 mg/day), and high interpatient variability." | ( Bardoxolone methyl (CDDO-Me) as a therapeutic agent: an update on its pharmacokinetic and pharmacodynamic properties. He, ZX; Wang, YY; Yang, YX; Zhe, H; Zhou, SF, 2014) | 1.85 |
| " Blood samples for pharmacokinetic analysis were taken over 120 hours following dose administration." | ( A food effect study and dose proportionality study to assess the pharmacokinetics and safety of bardoxolone methyl in healthy volunteers. Awni, WM; Dumas, EO; Kelley, RJ; Klein, CE; Meyer, CJ; Teuscher, NS, 2014) | 0.62 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Bardoxolone methyl is a potent, orally bioavailable Nrf-2 agonist." | ( A preliminary evaluation of bardoxolone methyl for the treatment of diabetic nephropathy. Thomas, M, 2012) | 1.58 |
| " These changes resulted in enhanced oral bioavailability and a superior pharmacodynamic effect in vivo." | ( Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy. Abou-Gharbia, M; Allaway, G; Biswal, S; Childers, W; Gordon, J; Jones, B; Korzekwa, K; Lounsbury, N; Mateo, G; Papaiahgari, S; Teijaro, C; Thimmulappa, RK; Ye, M, 2015) | 0.42 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " If mice were fed either the methyl ester or the ethyl amide derivative of the synthetic triterpenoid 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid (CDDO-ME and CDDO-EA, respectively), beginning 1 week after dosing with carcinogen, the number, size, and severity of lung carcinomas were markedly reduced." | ( The synthetic triterpenoids CDDO-methyl ester and CDDO-ethyl amide prevent lung cancer induced by vinyl carbamate in A/J mice. Dmitrovsky, E; Gribble, GW; Honda, T; Liby, K; Risingsong, R; Royce, DB; Sporn, MB; Sporn, TA; Williams, CR; Yore, MM, 2007) | 0.34 |
| " BARD at a dosage of 10mg/kg body weight was administered orally in drinking water." | ( Bardoxolone methyl prevents fat deposition and inflammation in the visceral fat of mice fed a high-fat diet. Camer, D; Dinh, CH; Huang, XF; Szabo, A; Wang, H; Yu, Y, 2015) | 1.86 |
| Class | Description |
|---|---|
| cyclohexenones | Any six-membered alicyclic ketone having one double bond in the ring. |
| [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 | 1.1709 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| TDP1 protein | Homo sapiens (human) | Potency | 1.1239 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| AR protein | Homo sapiens (human) | Potency | 10.9449 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743036; AID743042; AID743053; AID743054; AID743063 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 16.4580 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692; AID720719 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 4.8069 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743077; AID743078; AID743079; AID743080; AID743091 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 6.0070 | 0.0010 | 19.4141 | 70.9645 | AID743094 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 5.3080 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 21.1317 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| prostaglandin E2 receptor EP2 subtype | Homo sapiens (human) | Potency | 16.6261 | 0.1482 | 5.5312 | 35.2093 | AID743167 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 0.7660 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743066; AID743067 |
| Interferon beta | Homo sapiens (human) | Potency | 1.1709 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 8.3918 | 0.0023 | 19.5956 | 74.0614 | AID651631; AID720552 |
| ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 3.3491 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
| Ataxin-2 | Homo sapiens (human) | Potency | 3.3491 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
| [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) |
|---|---|---|---|---|---|---|---|
| Ubiquitin carboxyl-terminal hydrolase 2 | Homo sapiens (human) | IC50 (µMol) | 22.0000 | 5.4000 | 6.1000 | 6.8000 | AID1491550 |
| Ghrelin O-acyltransferase | Mus musculus (house mouse) | IC50 (µMol) | 0.0350 | 0.0350 | 0.1775 | 0.3200 | AID1639666 |
| Signal transducer and activator of transcription 3 | Homo sapiens (human) | IC50 (µMol) | 2.3800 | 0.0230 | 4.1378 | 9.9800 | AID1378642 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 200.0000 | 0.0009 | 1.9014 | 10.0000 | AID1465855 |
| Ubiquitin carboxyl-terminal hydrolase 7 | Homo sapiens (human) | IC50 (µMol) | 14.0800 | 0.1300 | 4.0462 | 8.0000 | AID1491549 |
| Ghrelin O-acyltransferase | Homo sapiens (human) | IC50 (µMol) | 14.5000 | 6.0000 | 7.5000 | 8.0000 | AID1639664; AID1802486 |
| [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) |
|---|---|---|---|---|---|---|---|
| Nuclear factor erythroid 2-related factor 2 | Homo sapiens (human) | EC50 (µMol) | 0.0600 | 0.0600 | 2.6167 | 9.9000 | AID1378643 |
| [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) |
|---|---|---|---|---|---|---|---|
| Nuclear factor erythroid 2-related factor 2 | Rattus norvegicus (Norway rat) | CD | 0.0005 | 0.0005 | 0.0005 | 0.0005 | AID1290523 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1200414 | Inhibition of BCRP protein expression in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1491549 | Inhibition of USP7 (unknown origin) using human N-terminal GST-tagged UBA52 as substrate preincubated for 10 mins followed by substrate addition measured after 45 mins by coomassie brilliant blue staining-based SDS-PAGE analysis | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2 | Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies. |
| AID1596419 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | |||
| AID1378644 | Activation of Nrf2 (unknown origin) expressed in human HaCaT-ARE-luc cells after 6 hrs by luciferase reporter gene assay relative to control tertbutylhydroquinone | 2017 | Journal of natural products, 08-25, Volume: 80, Issue:8 | Electrophilic Triterpenoid Enones: A Comparative Thiol-Trapping and Bioactivity Study. |
| AID1383486 | Induction of apoptosis in human A549/TR cells assessed as viable cells at 4.8 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 95.1%) | |||
| AID1200380 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as viable cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 90%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID248346 | Inhibitory concentration against proliferation of MCF-7 (ER Positive) breast cancer cells | 2004 | Journal of medicinal chemistry, Sep-23, Volume: 47, Issue:20 | Design, synthesis, and biological evaluation of biotin conjugates of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid for the isolation of the protein targets. |
| AID1200362 | Induction of apoptosis in human HCT8 cells assessed as late apoptotic cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 4.23%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1728762 | Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. |
| AID1465781 | Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as upregulation of NQO1 mRNA expression at 200 to 1000 nM after 48 hrs by quantitative RT-PCR analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465832 | Renoprotective activity in db/db mouse assessed as reduction in loss of foot processes at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by TEM microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383492 | Cell cycle arrest in human A549/TR cells assessed as accumulation at G0/G1 phase at 2.4 uM after 24 hrs by propidium iodide/RNase-staining based flow cytometric analysis (Rvb = 62.5%) | |||
| AID1307870 | Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as increase in GCLM mRNA expression at 100 nM incubated for 24 hrs in presence of NRF2 siRNA by qRT-PCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1307875 | Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as induction of NQO1 specific activity at 100 nM incubated for 48 hrs in presence of NRF2 siRNA by MTT reduction assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1290537 | Thiol reactivity using beta-mercaptoethanol assessed as chemical shifts at 25 degC by NMR spectroscopy | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1290519 | Binding affinity to recombinant mouse poly His-tagged Keap1 expressed in Escherichia coli assessed as chemical modification of Cys-273 residue incubated up to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1465866 | Drug level in Krebs buffer treated with 1-Hydroxyl-2-cyano-3-(4-(methyl-L-glutaminate-N5-yl)-benzyloxy)-12-oxo-oleana-2(3),9(11)-dien-28-oic Acid Methyl Ester assessed as bovine kidney GGT-mediated metabolite formation at 100 uM at pH 7.4 after 8 hrs in p | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1489877 | Pulmonary vasodilatory effect in MCT-induced Sprague-Dawley rat pulmonary arterial hypertension model assessed as mean pulmonary artery pressure at 2.1 ug/kg, inhaled daily for 28 days by polygraph method (Rvb = 30.63 +/- 1.16 mmHg) | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1424315 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of nitric oxide production | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Oleanane-, ursane-, and quinone methide friedelane-type triterpenoid derivatives: Recent advances in cancer treatment. |
| AID1465865 | Drug level in Krebs buffer treated with 1-Hydroxyl-2-cyano-3-(4-(methyl-L-glutaminate-N5-yl)-benzyloxy)-12-oxo-oleana-2(3),9(11)-dien-28-oic Acid Methyl Ester assessed as bovine kidney GGT-mediated metabolite formation at 100 uM at pH 7.4 after 8 hrs by H | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465823 | Antidiabetic nephropathic activity in db/db mouse assessed as increase in urinary creatinine at 0.65 mg/kg, ip administered thrice per week for 12 consecutive weeks measured at 24 hrs post 11 week administration | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1903909 | Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
| AID1200413 | Inhibition of MRP1 protein expression in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200429 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as body weight level at 59.4 umol/kg administered as via oral gavage daily for 21 days (Rvb = 20.8 +/- 2.2 g) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1139103 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Synthesis and cytotoxic activity of nitric oxide-releasing isosteviol derivatives. |
| AID1200379 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as necrotic cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 0.958%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1917366 | Inhibition of Pseudomonas aeruginosa RuvA expressed in Escherichia coli BL21(DE3) binding to HJ DNA assessed as reduction in RuvA-HJ DNA complex formation at >10 uM and measured after 15 mins using 5'-FAM labelled Holliday junction DNA as substrate by EMS | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1200396 | Inhibition of AKT protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200417 | Induction of nitrosylation of BCRP protein in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1378643 | Activation of Nrf2 (unknown origin) expressed in human HaCaT-ARE-luc cells after 6 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 08-25, Volume: 80, Issue:8 | Electrophilic Triterpenoid Enones: A Comparative Thiol-Trapping and Bioactivity Study. |
| AID1200448 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal color changes in kidney at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465870 | Drug level in Wistar rat liver homogenates treated with 1-Hydroxyl-2-cyano-3-(4-(methyl-L-glutaminate-N5-yl)-benzyloxy)-12-oxo-oleana-2(3),9(11)-dien-28-oic Acid Methyl Ester assessed as GGT-mediated metabolite formation at 100 uM after 8 hrs by HPLC anal | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID676568 | Cytotoxicity against C57BL/6 mouse BMDM cells assessed as LDH release after 24 hrs | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Synthesis, chemical reactivity as Michael acceptors, and biological potency of monocyclic cyanoenones, novel and highly potent anti-inflammatory and cytoprotective agents. |
| AID1465853 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200383 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as necrotic cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 0.958%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200460 | Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation at 1 uM after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1646255 | Inhibition of Keap1-Nrf2 Interaction in human HaCaT cells assessed as increase in Nrf2 protein level at 1 uM incubated for 16 hrs by Western blot analysis relative to control | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability. |
| AID1200398 | Inhibition of ERK protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200450 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal color changes in heart at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200455 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal weight changes in liver at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200361 | Induction of apoptosis in human HCT8 cells assessed as early apoptotic cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 1.21%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465804 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of COX2 mRNA expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by quantitative RT-PCR an | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200447 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal color changes in liver at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200345 | Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1290527 | Binding affinity to recombinant mouse poly His-tagged Keap1 expressed in Escherichia coli assessed as chemical modification of Cys-434 residue incubated up to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1465861 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of iNOS protein expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1489871 | Drug level in Sprague-Dawley rat lung treated with CDDO-NO at 1 mg/ml administered in trachea after 90 to 720 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1200377 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as early apoptotic cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 2.07%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383476 | Downregulation of Lon expression in human A549/TR cells at 4.8 uM after 24 hrs by Western blot analysis | |||
| AID1465833 | Renoprotective activity in db/db mouse assessed as reduction in mesangial expansion at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by TEM microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID224269 | Inhibition of nitric oxide (NO) production induced by interferon-gamma (IFN-gamma) in mouse macrophages | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | Synthetic oleanane and ursane triterpenoids with modified rings A and C: a series of highly active inhibitors of nitric oxide production in mouse macrophages. |
| AID1290538 | Thiol reactivity using N-acetyl cysteine assessed as chemical shifts at 25 degC by NMR spectroscopy | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1465812 | Anti-diabetic nephropathic activity in db/db mouse assessed as reduction in plasma urea nitrogen levels at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured 11 weeks post dose | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID676569 | Antiinflammatory activity in C57BL/6 mouse BMDM cells assessed as inhibition of LPS-stimulated TNFalpha production at 0.5 uM pretreated for 1 hr before LPS challenge after 8 to 24 hrs by immunoassay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Synthesis, chemical reactivity as Michael acceptors, and biological potency of monocyclic cyanoenones, novel and highly potent anti-inflammatory and cytoprotective agents. |
| AID1383485 | Induction of apoptosis in human A549/TR cells assessed as necrotic cells at 2.4 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.22%) | |||
| AID1910648 | Cytotoxicity against human ARPE-19 cells assessed as reduction in cell viability at 1 uM incubated for 96 hrs by MTT assay relative to control | 2022 | Journal of medicinal chemistry, 05-26, Volume: 65, Issue:10 | Phenyl Bis-Sulfonamide Keap1-Nrf2 Protein-Protein Interaction Inhibitors with an Alternative Binding Mode. |
| AID1200461 | Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation at 1 uM after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1581353 | Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | Discovery of Novel Celastrol Derivatives as Hsp90-Cdc37 Interaction Disruptors with Antitumor Activity. |
| AID1465837 | Half life in Sprague-Dawley rat at 10 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383474 | Induction of ROS generation in human A549/TR cells at 2.4 to 9.6 uM after 24 hrs by DCFH-DA dye-based flow cytometric analysis | |||
| AID1200395 | Inhibition of STAT3 protein phosphorylation in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1307865 | Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as increase in NQO1 mRNA expression at 100 nM incubated for 24 hrs in presence of non targeting siRNA by qRT-PCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1383469 | Induction of nitric oxide production in human A549/TR cells at 50 uM after 6 hrs by Griess assay | |||
| AID1200378 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as late apoptotic cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 0.95%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465864 | Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as increase in cytosolic NQO1 levels at 200 to 1000 nM after 48 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200449 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal color changes in lung at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200382 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as late apoptotic cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 0.95%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1491550 | Inhibition of USP2 (unknown origin) | 2018 | Journal of medicinal chemistry, 01-25, Volume: 61, Issue:2 | Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies. |
| AID1489865 | Drug uptake in Sprague-Dawley rat lung at 1 mg/ml administered in trachea after 60 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1307866 | Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as increase in GCLM mRNA expression at 100 nM incubated for 24 hrs in presence of non targeting siRNA by qRT-PCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1290525 | Cytotoxicity against rat H42E cells expressing ARE8L assessed as cellular ATP level after 24 hrs by Celltiter-Glo luminescent cell viability assay | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1465805 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of MCP1 mRNA expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by quantitative RT-PCR an | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1917355 | Inhibition of Bacillus subtilis RuvA/RuvB protein complex helicase activity expressed in Escherichia coli BL21(DE3) assessed as inhibition of HJ branch migration at 50 uM preincubated for 15 mins followed by substrate addition and measured after 1 hr usin | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1423732 | Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1465844 | Drug level in Sprague-Dawley rat heart at 20 mg/kg, ip measured at 90 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465821 | Anti-diabetic nephropathic activity in db/db mouse assessed as reduction in urinary albumin at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 24 hrs post 11 week administration | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID140447 | Inhibitory activity against production of nitric oxide induced by interferon gamma in mouse macrophages | 2002 | Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7 | A novel dicyanotriterpenoid, 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-onitrile, active at picomolar concentrations for inhibition of nitric oxide production. |
| AID1646256 | Inhibition of Keap1-Nrf2 Interaction in human HaCaT cells assessed as increase in NQO1 protein level at 1 uM incubated for 16 hrs by Western blot analysis relative to control | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability. |
| AID1200399 | Inhibition of ERK protein phosphorylation in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465798 | Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as activation of Nrf2 at 200 to 1000 nM after 48 hrs by ARE-driven luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200397 | Inhibition of AKT protein phosphorylation in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1489866 | Drug uptake in Sprague-Dawley rat lung at 1 mg/ml administered in trachea after 180 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1290523 | Induction of NRF2 activation in rat H42E cells expressing ARE8L assessed as reporter transgene activity after 24 hrs by luminescence assay | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID132692 | Inhibitory activity against production of nitric oxide induced by interferon-gamma in mouse macrophages | 1999 | Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24 | Novel synthetic oleanane triterpenoids: a series of highly active inhibitors of nitric oxide production in mouse macrophages. |
| AID1383482 | Induction of apoptosis in human A549/TR cells assessed as viable cells at 2.4 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 95.1%) | |||
| AID1465819 | Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as increase in nuclear to cytosolic Nfr2 ratio at 200 to 1000 nM after 48 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465839 | Volume of distribution at steady state in Sprague-Dawley rat at 10 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200360 | Induction of apoptosis in human HCT8 cells assessed as viable cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 92%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1596417 | Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | |||
| AID1465827 | Renoprotective activity in db/db mouse assessed as reduction in thickening of capillary walls in glomeruli at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by H/E-staining based microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465863 | Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as increase in cytosolic HO-1 levels at 200 to 1000 nM after 48 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465813 | Anti-diabetic nephropathic activity in db/db mouse assessed as reduction in plasma uric acid levels at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1290520 | Binding affinity to recombinant mouse poly His-tagged Keap1 expressed in Escherichia coli assessed as chemical modification of Cys-489 residue incubated up to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID589396 | Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Tricyclic compounds containing nonenolizable cyano enones. A novel class of highly potent anti-inflammatory and cytoprotective agents. |
| AID1383481 | Induction of apoptosis in human A549/TR cells assessed as necrotic cells at 1.2 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.22%) | |||
| AID1290535 | Binding affinity to recombinant human poly His-tagged GSTP1 expressed in Escherichia coli assessed as chemical modification at Cys-47 at 10:1 compound:protein molar ratio after 1 hr by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID589412 | Cytotoxicity against CD-1 mouse macrophages at 10 uM | 2011 | Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6 | Tricyclic compounds containing nonenolizable cyano enones. A novel class of highly potent anti-inflammatory and cytoprotective agents. |
| AID1064488 | Antiproliferative activity against mouse PANC1343 cells at 300 to 1000 nM after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and biological evaluation of amino acid methyl ester conjugates of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid against the production of nitric oxide (NO). |
| AID1423731 | Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1383491 | Cell cycle arrest in human A549/TR cells assessed as accumulation at G2/M phase at 1.2 uM after 24 hrs by propidium iodide/RNase-staining based flow cytometric analysis (Rvb = 24.7%) | |||
| AID1489883 | Pulmonary vasodilatory effect in MCT-induced Sprague-Dawley rat pulmonary arterial hypertension model assessed as right ventricular systolic pressure at 2.1 ug/kg, inhaled daily for 28 days co-administered with ISMN by polygraph method (Rvb = 56.09 +/- 3. | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1200456 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal weight changes in kidney at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200374 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as late apoptotic cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 0.95%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465807 | Toxicity in db/db mouse assessed as effect on water consumption at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured every other day | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200392 | Inhibition of HIF-1alpha protein expression in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465779 | Effect on Nfr2 mRNA expression in HEK293 cells harboring Keap1 at 200 to 1000 nM after 48 hrs by quantitative RT-PCR analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383480 | Induction of apoptosis in human A549/TR cells assessed as late apoptotic cells at 1.2 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.24%) | |||
| AID1139104 | Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9 | Synthesis and cytotoxic activity of nitric oxide-releasing isosteviol derivatives. |
| AID1465824 | Anti-diabetic nephropathic activity in db/db mouse assessed as reduction in urine albumin to creatinine ratio at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 24 hrs post 11 week administration | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383494 | Cell cycle arrest in human A549/TR cells assessed as accumulation at G0/G1 phase at 4.8 uM after 24 hrs by propidium iodide/RNase-staining based flow cytometric analysis (Rvb = 62.5%) | |||
| AID1489879 | Pulmonary vasodilatory effect in MCT-induced Sprague-Dawley rat pulmonary arterial hypertension model assessed as weight ratio of right ventricle to left ventricle and septum at 2.1 ug/kg, inhaled daily for 28 days (Rvb = 0.4796 +/- 0.030 No_unit) | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1200457 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal weight changes in lung at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383489 | Induction of apoptosis in human A549/TR cells assessed as necrotic cells at 4.8 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.22%) | |||
| AID1917352 | Inhibition of Pseudomonas aeruginosa RuvA/RuvB protein complex helicase activity expressed in Escherichia coli BL21(DE3) assessed as inhibition of HJ branch migration preincubated for 15 mins followed by substrate addition and measured after 1 hr using 5' | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1465869 | Drug level in Wistar rat plasma treated with 1-Hydroxyl-2-cyano-3-(4-(methyl-L-glutaminate-N5-yl)-benzyloxy)-12-oxo-oleana-2(3),9(11)-dien-28-oic Acid Methyl Ester assessed as GGT-mediated metabolite formation at 100 uM after 8 hrs by HPLC analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200415 | Induction of nitrosylation of P-gp protein in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200368 | Induction of apoptosis in human HCT8 cells assessed as viable cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 92%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1307879 | Cytoprotective activity in NHBE cells assessed as inhibition of tBHP-induced GSH depletion at 0.001 to 0.1 uM preincubated for 18 hrs followed by tBHP addition for 4 hrs by thiostar dye based fluorescence assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1917370 | Antimicrobial activity against Pseudomonas aeruginosa ATCC27853 assessed as colony formation at 50 uM preincubated for 1 hr followed by UV-light irradiation for 5 mins then culture on LB-agar plate for overnight by colony counting method | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1581354 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | Discovery of Novel Celastrol Derivatives as Hsp90-Cdc37 Interaction Disruptors with Antitumor Activity. |
| AID1378642 | Inhibition of IFN-gamma stimulated STAT3 (unknown origin) expressed in human HeLa cells after 6 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 08-25, Volume: 80, Issue:8 | Electrophilic Triterpenoid Enones: A Comparative Thiol-Trapping and Bioactivity Study. |
| AID1383487 | Induction of apoptosis in human A549/TR cells assessed as early apoptotic cells at 4.8 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.42%) | |||
| AID1917365 | Inhibition of Pseudomonas aeruginosa RuvA expressed in Escherichia coli BL21(DE3) binding to HJ DNA assessed as reduction in RuvA-HJ DNA complex formation at 40 uM and measured after 15 mins using 5'-FAM labelled Holliday junction DNA as substrate by EMSA | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1465789 | Solubility of compound in saline containing 1% 1,3-propylene glycol/ 1% Tween 80 at 100 uM at pH 7.4 by HPLC analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1423735 | Selectivity index, ratio of IC50 for HAF to IC50 for human HT-29 cells | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1383490 | Cell cycle arrest in human A549/TR cells assessed as accumulation at G0/G1 phase at 1.2 uM after 24 hrs by propidium iodide/RNase-staining based flow cytometric analysis (Rvb = 62.5%) | |||
| AID1465831 | Renoprotective activity in db/db mouse assessed as reduction in fused podocytes at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by TEM microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383495 | Cell cycle arrest in human A549/TR cells assessed as accumulation at G2/M phase at 4.8 uM after 24 hrs by propidium iodide/RNase-staining based flow cytometric analysis (Rvb = 24.7%) | |||
| AID1307869 | Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as increase in NQO1 mRNA expression at 100 nM incubated for 24 hrs in presence of NRF2 siRNA by qRT-PCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1903908 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
| AID1290521 | Binding affinity to recombinant mouse poly His-tagged Keap1 expressed in Escherichia coli assessed as chemical modification of Cys-257 residue incubated up to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1378641 | Inhibition of TNF-alpha stimulated NF-kappaB (unknown origin) expressed in mouse NIH/3T3 cells after 6 hrs by luciferase reporter gene assay | 2017 | Journal of natural products, 08-25, Volume: 80, Issue:8 | Electrophilic Triterpenoid Enones: A Comparative Thiol-Trapping and Bioactivity Study. |
| AID1423729 | Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1465862 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as mitigation of TNFalpha-induced increase in ratio of nuclear to cytosolic p65 at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465840 | Cmax in Sprague-Dawley rat at 10 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1917356 | Inhibition of Thermus thermophilus RuvA/RuvB protein complex helicase activity expressed in Escherichia coli BL21(DE3) assessed as inhibition of HJ branch migration at 50 uM preincubated for 15 mins followed by substrate addition and measured after 1 hr u | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1903910 | Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
| AID1581351 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | Discovery of Novel Celastrol Derivatives as Hsp90-Cdc37 Interaction Disruptors with Antitumor Activity. |
| AID1200364 | Induction of apoptosis in human HCT8 cells assessed as viable cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 92%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383488 | Induction of apoptosis in human A549/TR cells assessed as late apoptotic cells at 4.8 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.24%) | |||
| AID1465788 | Solubility of compound in saline at 100 uM at pH 7.4 by HPLC analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465780 | Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as upregulation of HO-1 mRNA expression at 200 to 1000 nM after 48 hrs by quantitative RT-PCR analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200346 | Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200393 | Inhibition of HIF-1alpha protein expression in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200367 | Induction of apoptosis in human HCT8 cells assessed as necrotic cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 2.58%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1489872 | Drug level in Sprague-Dawley rat plasma treated with CDDO-NO at 1 mg/ml administered in trachea after 15 to 720 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1465802 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as TNFalpha-induced NFkappaB activation at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by NFkappaB-driven luciferase reporter gene assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200381 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as early apoptotic cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 2.07%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200452 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal size changes in kidney at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383464 | Antiproliferative activity against human A549/TR cells after 72 hrs by MTT assay | |||
| AID1465871 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of MCP1 protein expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465826 | Renoprotective activity in db/db mouse assessed as increase in number of intraglomerular mesangial cells at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by H/E-staining based microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465835 | AUC (0 to t) in Sprague-Dawley rat at 10 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1917358 | Inhibition of HJ-DNA dependent Pseudomonas aeruginosa RuvB ATPase activity expressed in Escherichia coli BL21(DE3) assessed as inhibition of ATP hydrolysis preincubated at 40 uM followed by ATP addition and measured after 1 hr by Kinase-Glo reagent based | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1200375 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as necrotic cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 0.958%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200370 | Induction of apoptosis in human HCT8 cells assessed as late apoptotic cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 4.23%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465855 | Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by patch clamp assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200376 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as viable cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 90%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465842 | Drug level in Sprague-Dawley rat liver at 20 mg/kg, ip measured at 90 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383484 | Induction of apoptosis in human A549/TR cells assessed as late apoptotic cells at 2.4 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 1.24%) | |||
| AID1200412 | Inhibition of P-gp protein expression in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383470 | Induction of nitric oxide production in human MRC5 cells at 50 uM after 6 hrs by Griess assay | |||
| AID1646258 | Inhibition of Keap1-Nrf2 Interaction in human HaCaT cells assessed as increase in Nrf2 protein level at 0.25 uM incubated for 16 hrs by Western blot analysis relative to control | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability. |
| AID1290522 | Stabilization of NRF2 in rat H42E cells expressing ARE8L at 0.01 to 30 nM after 1 hr by Western blot analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1465841 | Drug level in Sprague-Dawley rat kidney at 20 mg/kg, ip measured at 90 mins by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200365 | Induction of apoptosis in human HCT8 cells assessed as early apoptotic cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 1.21%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465834 | Renoprotective activity in db/db mouse assessed as reduction in glomerular basement thickening at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by TEM microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200394 | Inhibition of STAT3 protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383466 | Resistant factor, ratio of IC50 for human A549/TR cells to IC50 for human A549 cells | |||
| AID1383479 | Induction of apoptosis in human A549/TR cells assessed as early apoptotic cells at 1.2 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.42%) | |||
| AID1200432 | Antitumor activity against FU-resistant human HCT8 cells xenografted in nude BALB/c mouse assessed as reduction in tumor weight at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1423734 | Selectivity index, ratio of IC50 for HAF to IC50 for human HCT116 cells | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1465838 | Clearance in Sprague-Dawley rat at 10 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465860 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of COX2 protein expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1581352 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | 2019 | Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23 | Discovery of Novel Celastrol Derivatives as Hsp90-Cdc37 Interaction Disruptors with Antitumor Activity. |
| AID1200372 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as viable cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 90%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1383493 | Cell cycle arrest in human A549/TR cells assessed as accumulation at G2/M phase at 2.4 uM after 24 hrs by propidium iodide/RNase-staining based flow cytometric analysis (Rvb = 24.7%) | |||
| AID1536357 | Activation of Keap1/Cul3/Nrf2 in human BEAS2B cells assessed as increase in NQO1 levels measured after 48 hrs | 2019 | Bioorganic & medicinal chemistry, 02-15, Volume: 27, Issue:4 | Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo. |
| AID1917368 | Antimicrobial activity against Pseudomonas aeruginosa ATCC27853 assessed as colony formation at 50 uM preincubated for 1 hr then culture on LB-agar plate for overnight by colony counting method | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Identification of small-molecule inhibitors of the DNA repair proteins RuvAB from Pseudomonas aeruginosa. |
| AID1903911 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | |||
| AID1465806 | Toxicity in db/db mouse assessed as effect on food consumption at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured every other day | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465854 | Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1383465 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | |||
| AID1465857 | Acute toxicity in ip dosed ICR mouse assessed as lethality administered daily for 7 days | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200371 | Induction of apoptosis in human HCT8 cells assessed as necrotic cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 2.58%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1290528 | Binding affinity to recombinant mouse poly His-tagged Keap1 expressed in Escherichia coli assessed as chemical modification of Cys-613 residue incubated up to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1465808 | Toxicity in db/db mouse assessed as increase in body weight at 0.65 mg/kg, ip administered thrice per week for 12 consecutive weeks measured every other day (Rvb = 15%) | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1241432 | Activation of Nrf2 in human BEAS2B cells assessed as increase in HO1 gene expression at 10 uM incubated for 6 hrs by qPCR method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy. |
| AID1646259 | Inhibition of Keap1-Nrf2 Interaction in human HaCaT cells assessed as increase in NQO1 protein level at 0.25 uM incubated for 16 hrs by Western blot analysis relative to control | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability. |
| AID1200451 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal size changes in liver at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465856 | Inhibition of human ERG expressed in CHO cells at 200 uM at -80 mV holding potential by patch clamp assay relative to control | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465859 | Cardioprotective activity in C57BL/6 db/db mouse assessed as reduction in apoptotic cardiomyocyte levels at 0.65 mg/kg, ip administered for 12 weeks by TUNNEL assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200458 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal weight changes in heart at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1423730 | Inhibition of Bmi1 protein expression in human HCT116 cells after 8 hrs by Western blot analysis | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1423733 | Antiproliferative activity against HAF after 72 hrs by SRB assay | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1465814 | Anti-diabetic nephropathic activity in db/db mouse assessed as reduction in plasma creatinine levels at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1465836 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, iv measured up to 24 hrs by LC-MS/MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200416 | Induction of nitrosylation of MRP1 protein in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465867 | Drug level in Wistar rat kidney homogenates treated with 1-Hydroxyl-2-cyano-3-(4-(methyl-L-glutaminate-N5-yl)-benzyloxy)-12-oxo-oleana-2(3),9(11)-dien-28-oic Acid Methyl Ester assessed as GGT-mediated metabolite formation at 100 uM after 8 hrs by HPLC ana | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1596418 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | |||
| AID1465825 | Renoprotective activity in db/db mouse assessed as reduction of fibrosis in glomeruli at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by H/E-staining based microscopic analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200369 | Induction of apoptosis in human HCT8 cells assessed as early apoptotic cells level at 1 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 1.21%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1290526 | Binding affinity to recombinant mouse poly His-tagged Keap1 expressed in Escherichia coli assessed as chemical modification of Cys-288 residue incubated up to 24 hrs by LC-MS/MS analysis | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | Design and Synthesis of Irreversible Analogues of Bardoxolone Methyl for the Identification of Pharmacologically Relevant Targets and Interaction Sites. |
| AID1383478 | Induction of apoptosis in human A549/TR cells assessed as viable cells at 1.2 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 95.1%) | |||
| AID1200363 | Induction of apoptosis in human HCT8 cells assessed as necrotic cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 2.58%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1200453 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal size changes in lung at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1489882 | Pulmonary vasodilatory effect in MCT-induced Sprague-Dawley rat pulmonary arterial hypertension model assessed as mean pulmonary artery pressure at 2.1 ug/kg, inhaled daily for 28 days co-administered with ISMN by polygraph method (Rvb = 30.63 +/- 1.16 mm | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1489884 | Pulmonary vasodilatory effect in MCT-induced Sprague-Dawley rat pulmonary arterial hypertension model assessed as weight ratio of right ventricle to left ventricle and septum at 2.1 ug/kg, inhaled daily for 28 days co-administered with ISMN (Rvb = 0.4796 | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1423736 | Selectivity index, ratio of IC50 for HAF to IC50 for human HCT8 cells | 2018 | ACS medicinal chemistry letters, Nov-08, Volume: 9, Issue:11 | Synthesis of Cyanoenone-Modified Diterpenoid Analogs as Novel Bmi-1-Mediated Antitumor Agents. |
| AID1383483 | Induction of apoptosis in human A549/TR cells assessed as early apoptotic cells at 2.4 uM after 24 hrs by Annexin-V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 3.42%) | |||
| AID1728767 | Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. |
| AID1200366 | Induction of apoptosis in human HCT8 cells assessed as late apoptotic cells level at 0.5 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 4.23%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1307874 | Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as induction of NQO1 specific activity at 100 nM incubated for 48 hrs in presence of non targeting siRNA by MTT reduction assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. |
| AID1064489 | Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of tBHP-induced ROS production at 100 nM pretreated for 18 hrs before challenge measured after 15 mins by H2DCFA-based flow cytometry | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2 | Synthesis and biological evaluation of amino acid methyl ester conjugates of 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid against the production of nitric oxide (NO). |
| AID1200344 | Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465817 | Anti-diabetic nephropathic activity in db/db mouse assessed as reduction in 24 hr urine volume at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID1200373 | Induction of apoptosis in FU-resistant human HCT8 cells assessed as early apoptotic cells level at 0.25 uM incubated for 24 hrs by FITC-Annexin-V and propidium iodide staining based flow cytometry (Rvb = 2.07%) | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1465803 | Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of iNOS mRNA expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by quantitative RT-PCR an | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21 | Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy. |
| AID676573 | Induction of apoptosis in LPS-stimulated C57BL/6 mouse BMDM cells assessed as LDH release at 0.5 uM pretreated for 1 hr before LPS challenge after 24 hrs | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Synthesis, chemical reactivity as Michael acceptors, and biological potency of monocyclic cyanoenones, novel and highly potent anti-inflammatory and cytoprotective agents. |
| AID1489870 | Drug uptake in Sprague-Dawley rat lung at 1 mg/ml administered in trachea after 360 mins by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| AID1200454 | Toxicity in nude BALB/c mouse xenografted with FU-resistant human HCT8 cells assessed as abnormal size changes in heart at 59.4 umol/kg administered as via oral gavage daily for 21 days | 2015 | Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5 | Synthesis of CDDO-amino acid-nitric oxide donor trihybrids as potential antitumor agents against both drug-sensitive and drug-resistant colon cancer. |
| AID1489878 | Pulmonary vasodilatory effect in MCT-induced Sprague-Dawley rat pulmonary arterial hypertension model assessed as right ventricular systolic pressure at 2.1 ug/kg, inhaled daily for 28 days by polygraph method (Rvb = 56.09 +/- 3.24 mmHg) | 2018 | Journal of medicinal chemistry, 02-22, Volume: 61, Issue:4 | Identification of a Novel Hybridization from Isosorbide 5-Mononitrate and Bardoxolone Methyl with Dual Activities of Pulmonary Vasodilation and Vascular Remodeling Inhibition on Pulmonary Arterial Hypertension Rats. |
| 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. |
| AID1645848 | NCATS Kinetic Aqueous Solubility Profiling | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14 | Predictive models of aqueous solubility of organic compounds built on A large dataset of high integrity. |
| 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. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1346800 | Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors) | 2000 | Molecular endocrinology (Baltimore, Md.), Oct, Volume: 14, Issue:10 | A synthetic triterpenoid, 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), is a ligand for the peroxisome proliferator-activated receptor gamma. |
| AID1802486 | GOAT Activity Assay from Article 10.1021/acs.biochem.6b01008: \\Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.\\ | 2017 | Biochemistry, 02-21, Volume: 56, Issue:7 | Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation. |
| [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 | 1 (0.43) | 18.2507 |
| 2000's | 30 (12.77) | 29.6817 |
| 2010's | 164 (69.79) | 24.3611 |
| 2020's | 40 (17.02) | 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 (44.84) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 18 (7.59%) | 5.53% |
| Reviews | 25 (10.55%) | 6.00% |
| Case Studies | 1 (0.42%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 193 (81.43%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||