Assay ID | Title | Year | Journal | Article |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3
| High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
| Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID1741898 | Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c nude mouse assessed as reduction in tumor weight at 10 mg/kg, ip measured at 2 days interval for 21 days relative to control | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1430073 | Lipophilicity, log D of compound at pH 7.4 | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1564517 | Inhibition of rat TrxR1 using DTNB as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1741863 | Antiproliferative activity against human MCF7 cells after 72 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1392921 | Growth inhibition of human DU145 cells after 48 hrs by WST-1 assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1433268 | Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1455312 | Cytotoxicity against human HCT116 cells at 2 to 50 nM after 24 to 48 hrs in presence of TGF-beta1 by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1392923 | Growth inhibition of human LNCAP cells after 48 hrs by WST-1 assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1741864 | Antiproliferative activity against human A549 cells after 72 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1433254 | Antiproliferative activity against p53 null human U937 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1392946 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 3 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1474919 | Antiproliferative activity against human U2OS cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1173277 | Cytotoxicity against mouse RAW264.7 cells assessed as cell proliferation at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents. |
AID1206053 | Induction of ROS production in human A549 cells after 3 hrs by APF staining-based fluorescence assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1158951 | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1677560 | Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by MTT assay | | | |
AID1396583 | Toxicity in po dosed mouse | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. |
AID1474915 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1459286 | Induction of bovine tubulin depolymerization at 25 uM measured every 30 secs for 60 mins by spectrophotometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1392947 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 7 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1455335 | Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455310 | Antimigratory activity in human HCT116 cells assessed as inhibition of TGF-beta1-induced cell migration at 50 nM after 48 hrs by trans-well assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1564518 | Inhibition of TrxR1 (unknown origin) using DTNB as substrate preincubated for 30 mins in presence of insulin followed by substrate addition by colorimetry | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1564522 | Cytotoxicity against human PBMC assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1433260 | Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1206058 | Reduction in reduced GSH level in human A549 cells at 10 uM after 4 hrs by luminescence assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1377676 | Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1426165 | Inhibition of equine liver GST assessed as decrease in conjugation of CDNB to GSH at 100 uM preincubated with GSH for 30 mins followed by CDNB addition measured for 3 mins relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy. |
AID1455323 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1168752 | Selectivity ratio of IC50 for human HaCaT cells to IC50 for human PANC1 cells | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness. |
AID1741881 | Induction of autophagy in human MDA-MB-231 cells transfected with mRFP-eGFP-LC3 assessed as accumulation of autophagosomes by measuring increase in red fluorescence at 1.8 uM measured after 24 hrs by confocal laser scanning microscopy | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1392949 | Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 3 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1229943 | Cytotoxicity against rat PC12 cells assessed as reduction in cell viability at 20 uM to 100 uM incubated for 24 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Synthesis of piperlongumine analogues and discovery of nuclear factor erythroid 2-related factor 2 (Nrf2) activators as potential neuroprotective agents. |
AID1433250 | Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433233 | Induction of apoptosis in p53 null human U937 cells assessed as PARP-1 cleavage at 2 uM after 24 hrs in presence of SAHA by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1677584 | Inhibition of mTOR phosphorylation in human BEL-7402/5-FU cells at 2 uM incubated for 72 hrs by Western blot analysis | | | |
AID1677557 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay | | | |
AID1206041 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1433306 | Effect on SAHA-induced apoptosis in p53 null human U937 cells assessed as decrease in XIAP expression level by measuring ratio of XIAP to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1206045 | Antiproliferative activity against human HaCaT cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1455321 | Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1459266 | Induction of apoptosis in human MCF7 cells assessed as downregulation of Bcl2 expression at 10 uM after 48 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1474938 | Induction of apoptosis in human HCT116 cells after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1433256 | Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1392948 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 10 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1551745 | Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1455345 | Induction of ROS accumulation in human HCT116 cells at 10 uM after 3 hrs by DCFH-DA staining-based fluorescence microscopic analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455316 | Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered daily for 21 consecutive days relative to control | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433247 | Induction of apoptosis in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant at 1 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1455339 | Cmax in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433234 | Induction of cell death in p53 null human U937 cells at 1 to 4 uM after 24 hrs by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1173275 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 10 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents. |
AID1433236 | Induction of cell death in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant assessed as combination index at 1 to 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1392950 | Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 7 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1433296 | Induction of DNA damage in p53 null human U937 cells assessed as increase in gammaH2AX expression level by measuring ratio of gammaH2AX to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1392925 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells by Western blot analysis | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1474920 | Antiproliferative activity against human Saos2 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1392931 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 5 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1455367 | Inhibition of IL-1beta-mediated adhesion of human rhodamine 123-labeled HCT116 cells to HUVEC at 50 nM after 1 hr by fluoresence assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433232 | Induction of apoptosis in p53 null human U937 cells assessed as caspase 3 cleavage at 2 uM after 24 hrs in presence of SAHA by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433244 | Induction of apoptosis in p53 null human U937 cells at 1 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433305 | Effect on SAHA-induced apoptosis in p53 null human U937 cells assessed as increase in Bim EL expression level by measuring ratio of Bim EL to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433301 | Induction of DNA damage in p53 null human U937 cells assessed as decrease in CHK1 expression level by measuring ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1677566 | Inhibition of TrxR in human BEL-7402/5-FU cells by colorimetric assay | | | |
AID1455377 | Inhibition of TGF-beta1-induced increase in expression levels of vimentin protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455328 | Antiproliferative activity against human K562 cells after 72 hrs in presence of ligustrazine by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1276122 | Cytotoxicity against human SF188 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1551762 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation at 150 uM preincubated for 3 mins followed by collagen addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1276118 | Cytotoxicity against human T98G cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1455346 | Induction of ROS accumulation in human CCD-841 cells at 10 uM after 3 hrs by DCFH-DA staining-based fluorescence microscopic analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1426174 | Electrophilicity of the compound assessed as second-oder rate constant for reaction with cysteamine under pseudo-first-oder condition at 40 uM by spectrophotometric method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy. |
AID1433269 | Antiproliferative activity against Ara-C resistant human CMK cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433270 | Inhibition of HDAC in p53 null human U937 cells assessed as hyper acetylation of histone H4 at 1 uM after 4 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459275 | Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 20 uM after 24 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1551764 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of PAF-induced platelet aggregation at 150 uM preincubated for 3 mins followed by PAF addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1551755 | Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida albicans ATCC 10231 | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1433287 | Cytotoxicity against p53 null human U937 cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1158950 | Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1174985 | Cytotoxicity against human MA9.3 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
| Design of a hydrogen peroxide-activatable agent that specifically targets cancer cells. |
AID1433266 | Antiproliferative activity against human MOLM13 cells harboring wild type p53/FLT3-ITD mutant after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459305 | Effect on tubulin polymerization in human MCF7 cells at 1 | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1433297 | Effect on SAHA-induced DNA damage in p53 null human U937 cells assessed as increase in gammaH2AX expression level by measuring ratio of gammaH2AX to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1677583 | Inhibition of AKT phosphorylation in human BEL-7402/5-FU cells at 2 uM incubated for 72 hrs by Western blot analysis | | | |
AID1433304 | Induction of apoptosis in p53 null human U937 cells assessed as decrease in XIAP expression level by measuring ratio of XIAP to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1168750 | Cytotoxicity against human PANC1 cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness. |
AID1433255 | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1474931 | Induction of apoptosis in human Saos2 cells at 5 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID336829 | Cytotoxicity against human A549 cells after 6 days by MTT assay | | | |
AID1551742 | Antifungal activity against Candida glabrata ATCC 90030 after 24 hrs by CLSI broth microdilution method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1433299 | Upregulation of Rad51 protein expression in p53 null human U937 cells assessed as ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1276119 | Cytotoxicity against human HT1080 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1677572 | Induction of autophagy in human BEL-7402/5-FU cells expressing mRFP-eGFP-LC3 assessed as autophagosomes at 2 uM after 24 hrs by confocal laser scanning microscopic method | | | |
AID1677561 | Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability after 72 hrs by MTT assay | | | |
AID1392935 | Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 5 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1455379 | Inhibition of TGF-beta1-induced increase in expression levels of snail protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433261 | Antiproliferative activity against human OCI-AML3 cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433262 | Antiproliferative activity against human CMS cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1916768 | Cytotoxicity against human HCT-116 incubated for 24 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy. |
AID1741868 | Inhibition of TrxR in human MDA-MB-231 cells measured after 72 hrs by colorimetric method | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1459280 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 5 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1459273 | Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 1 to 20 uM in presence of N-acetyl cysteine after 48 hrs by alamarBlue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1474941 | Cell cycle arrest in human HCT116 cells decrease in population at G0/G1 phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1741866 | Antiproliferative activity against human KB-VIN cells after 72 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1206044 | Antiproliferative activity against HFF1 cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1455324 | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1392934 | Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 1 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1741862 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1459299 | Induction of reactive oxygen species generation in human MCF7 cells assessed as decrease in cell viability at 1 to 20 uM in presence of trolox after 48 hrs by alamarBlue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1455349 | Antiproliferative activity against human HCT116 cells at 8 uM after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1459296 | Binding affinity to colchicine-binding site of beta tubulin in human HT-29 cells assessed as inhibition of formation of protein-N,N'-Ethylene-bis(iodoacetamide) adduct at 40 uM after 2 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1377679 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1741865 | Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1455380 | Inhibition of TGF-beta1-induced increase in expression levels of twist protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433263 | Antiproliferative activity against human CMK cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1455338 | Half life in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433257 | Antiproliferative activity against human CMY cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1229947 | Cytotoxicity against rat PC12 cells assessed as reduction in cell viability at 20 uM incubated for 24 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Synthesis of piperlongumine analogues and discovery of nuclear factor erythroid 2-related factor 2 (Nrf2) activators as potential neuroprotective agents. |
AID1393006 | Growth inhibition of human PC3 cells after 24 to 48 hrs by WST-1 assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1433272 | Effect on SAHA-induced HDAC inhibition in p53 null human U937 cells assessed as hyper acetylation of histone H4 at 1 uM after 4 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459291 | Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1474933 | Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1158948 | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1276115 | Cytotoxicity against human SKBR3 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1455341 | Volume of distribution at steady state in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1392922 | Growth inhibition of human PC3 cells after 48 hrs by WST-1 assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1459304 | Induction of tubulin depolymerization in human Jurkat cells at 5 to 20 uM after 4 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1741871 | Induction of reactive oxygen species generation in human MDA-MB-231 cells measured after 24 hrs by DCFH-DA probe based flow cytometry | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1396584 | Senolytic activity against non-senescent human WI38 cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. |
AID1474930 | Induction of apoptosis in human Saos2 cells at 1 uM after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1551760 | Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Staphylococcus aureus ATCC 6538 | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1433285 | Cytotoxicity against human MCF10A cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1474935 | Cell cycle arrest in human Saos2 cells assessed as accumulation at S phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1474934 | Cell cycle arrest in human Saos2 cells assessed as accumulation at G2/M phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1396586 | Selectivity index, ratio of EC50 for non-senescent human WI38 cells to EC50 for ionizing radiation induced human WI38 senescent cells | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. |
AID1564521 | Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1551758 | Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida glabrata ATCC 90030 | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1433267 | Antiproliferative activity against human HL60 cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459285 | Induction of apoptosis in human MCF7 cells assessed as downregulation of Mcl-1 expression at 10 uM after 72 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1455320 | Solubility of compound in phosphate buffer at pH 7.4 after 8 hrs by HPLC analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1677574 | Induction of autophagy in human BEL-7402/5-FU cells expressing mRFP-eGFP-LC3 assessed as auto lysosomes at 2 uM after 24 hrs by confocal laser scanning microscopic method | | | |
AID1392930 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells assessed as ratio of phosphorylated STAT3 protein level to GAPDH protein level at 1 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1741886 | Induction of autophagy in human MDA-MB-231 cells transfected with mRFP-eGFP-LC3 assessed as increase in LC3-II expression at 1.8 uM measured after 72 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1459272 | Cytotoxicity in human MCF10A cells at 10 uM after 24 to 48 hrs by alamarBlue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1433271 | Inhibition of HDAC6 in p53 null human U937 cells assessed as hyper acetylation of alpha tubulin at 1 uM after 4 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433259 | Antiproliferative activity against Ara-C resistant human HL60 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1741874 | Induction of apoptosis in human MDA-MB-231 cells at 1.8 uM measured after 72 hrs by APC-Annexin V/7-AAD staining based flow cytometry relative to control | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1455336 | Antiproliferative activity against human CCD-841 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1158949 | Cytotoxicity against human ZR75-30 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1433295 | Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs in presence of SAHA by SYBR gold staining based alkaline comet assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459294 | Binding affinity to colchicine-binding site of beta tubulin in human MCF7 cells assessed as inhibition of formation of protein-N,N'-Ethylene-bis(iodoacetamide) adduct at 40 uM after 2 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1206040 | Antiproliferative activity against human A375 cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1168751 | Cytotoxicity against human HaCaT cells assessed as reduction in cell viability after 24 hrs by MTT reduction assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | A new goniothalamin N-acylated aza-derivative strongly downregulates mediators of signaling transduction associated with pancreatic cancer aggressiveness. |
AID1459274 | Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 20 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1433258 | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1551748 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation at 300 uM preincubated for 3 mins followed by collagen addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1551759 | Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida parapsilosis ATCC 22019 | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1430070 | Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1433294 | Induction of DNA damage in p53 null human U937 cells at 2 uM after 20 hrs by SYBR gold staining based alkaline comet assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433292 | Induction of apoptosis in p53 null human U937 cells at 2 uM preincubated with NAC for 3 hrs followed by compound addition measured after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1377681 | Antiproliferative activity against human A549 cells at 10 uM after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1377683 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1173278 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents. |
AID1430075 | Permeability of the compound at pH 7.4 | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1433249 | Induction of apoptosis in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant at 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1396588 | Induction of ROS production in ionizing radiation induced human WI38 senescent cells up to 64 uM after 1.5 hrs by DHR123 dye based flow cytometry | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. |
AID1455376 | Inhibition of TGF-beta1-induced decrease in expression levels of E-cadherin protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1173274 | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 1 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents. |
AID1433303 | Induction of apoptosis in p53 null human U937 cells assessed as increase in Bim EL expression level by measuring ratio of Bim EL to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433291 | Induction of apoptosis in p53 null human U937 cells at 2 uM preincubated with NAC for 3 hrs followed by compound addition measured after 24 hrs by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459278 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 10 uM after 24 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1433248 | Induction of apoptosis in human MOLM13 cells harboring wild type p53/FLT3-ITD mutant at 2 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459307 | Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1276116 | Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1677559 | Cytotoxicity against human BEL-7402/5-FU cells assessed as reduction in cell viability after 72 hrs by MTT assay | | | |
AID1433273 | Effect on SAHA-induced HDAC6 inhibition in p53 null human U937 cells assessed as hyper acetylation of alpha tubulin at 1 uM after 4 hrs by Western blot analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1158953 | Cytotoxicity against human WI38 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1551749 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation at 300 uM preincubated for 3 mins followed by arachidonic acid addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1206052 | Induction of ROS production in human A549 cells after 3 hrs by DHE staining-based fluorescence assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1377684 | Cytotoxicity against human CCD-841 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1741861 | Inhibition of purified rat liver TrxR measured after 75 mins in presence of NADPH by DTNB based assay | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1433245 | Induction of apoptosis in p53 null human U937 cells at 2 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1728183 | Cytotoxicity against rat PC12 cells at 50 uM by MTT assay | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Identification and optimization of piperlongumine analogues as potential antioxidant and anti-inflammatory agents via activation of Nrf2. |
AID1459292 | Induction of microtubule depolymerization in human MCF7 cells at 10 uM after 16 hrs by immunofluorescence analysis | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1474940 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 1 to 5 uM after 24 hrs by propidium iodide staining based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1433252 | Antiproliferative activity against human CMK cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1377677 | Aqueous solubility of the compound in pure water by HPLC analysis | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1459268 | Antiproliferative activity in human Jurkat cells assessed as cell viability after 48 hrs by alamarBlue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1433284 | Cytotoxicity against human MCF10A cells assessed as decrease in cell viability at 0.5 to 5 uM after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1455388 | Inhibition of TGF-beta1-regulated increase in nuclear beta-catenin in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1206046 | Antiproliferative activity against human MCF10A cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1741882 | Induction of autophagy in human MDA-MB-231 cells transfected with mRFP-eGFP-LC3 assessed as accumulation of autolysosome by measuring increase in red fluorescence at 1.8 uM measured after 24 hrs by confocal laser scanning microscopy | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1433251 | Antiproliferative activity against human CMS cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1229945 | Cytotoxicity against human L02 cells assessed as reduction in cell viability at 20 uM to 100 uM incubated for 24 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Synthesis of piperlongumine analogues and discovery of nuclear factor erythroid 2-related factor 2 (Nrf2) activators as potential neuroprotective agents. |
AID1455333 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1474939 | Induction of apoptosis in human Saos2 cells after 24 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1459821 | Inhibition of NF-kappaB in human A549 cells after 24 hrs by luciferase reporter gene assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis of coumaperine derivatives: Their NF-κB inhibitory effect, inhibition of cell migration and their cytotoxic activity. |
AID1377687 | Antitumor activity against human HCT116 cells xenografted in BALB/c nude mouse assessed as reduction in tumor weight at 5 mg/kg, ip administered daily for 21 days | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1433264 | Antiproliferative activity against p53 null human U937 cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1741878 | Induction of apoptosis in human MDA-MB-231 cells assessed as activation of caspase-3 cleavage at 1.8 uM measured after 72 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1459283 | Cell cycle arrest in human MCF7 cells assessed as sub G0/G1 phase accumulation at 10 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1392927 | Inhibition of STAT3 phosphorylation at Tyr705 residues in human DU145 cells after 24 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1455384 | Inhibition of TGF-beta1-induced GSK-3beta phosphorylation in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1564516 | Inhibition of TrxR in human SH-SY5Y cells using DTNB as substrate preincubated for 15 mins followed by substrate addition and measured for 20 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1677558 | Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay | | | |
AID1377680 | Antiproliferative activity against human HCT116 cells at 10 uM after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1455327 | Antiproliferative activity against human A549 cells after 72 hrs in presence of ligustrazine by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1459281 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 10 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1433302 | Effect on SAHA-induced DNA damage in p53 null human U937 cells assessed as decrease in CHK1 expression level by measuring ratio of CHK1 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1433265 | Antiproliferative activity against human MV4-11 cells after 72 hrs in presence of SAHA by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1206043 | Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1459284 | Cell cycle arrest in human MCF7 cells assessed as sub G0/G1 phase accumulation at 20 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1430068 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1433235 | Induction of cell death in p53 null human U937 cells assessed as combination index at 2 to 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1206042 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1396587 | Induction of OXR1 degradation in ionizing radiation induced human WI38 senescent cells at 5 uM after 24 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. |
AID1276117 | Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1430069 | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1455340 | Clearance in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433246 | Induction of apoptosis in p53 null human U937 cells at 4 uM after 24 hrs in presence of SAHA by annexin V-FITC/PI staining based flow cytometry | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1459290 | Disruption of microtubule network in human MCF7 cells at 20 uM after 16 hrs by immunofluorescence analysis | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1158947 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1589252 | Inhibition of MAPK/NFkappaB in ICR mouse RAW264.7 cells assessed as reduction in LPS-induced IL6 production at 10 uM pretreated for 0.5 hrs followed by LPS challenge and measured after 24 hrs by ELISA relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI). |
AID1564523 | Cytotoxicity against human HaCaT assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1459279 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 15 uM after 24 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1430067 | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1459306 | Effect on tubulin polymerization in human Jurkat cells at 1 | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID336831 | Cytotoxicity against human KB cells after 3 days by MTT assay | | | |
AID1474923 | Induction of reactive oxygen species generation in human Saos2 cells at 10 uM after 1 hr by DCFH-DA dye-based fluorescence microscopic analysis relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1551741 | Antifungal activity against Candida krusei ATCC 6258 after 24 hrs by CLSI broth microdilution method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1459282 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 15 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1174984 | Selectivity ratio of IC50 for human primary CD34+ blood stem cells to IC50 for human MA9.3 cells | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
| Design of a hydrogen peroxide-activatable agent that specifically targets cancer cells. |
AID1474916 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1455325 | Antiproliferative activity against human U87MG cells after 72 hrs in presence of ligustrazine by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1551751 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation at 300 uM preincubated for 3 mins followed by thrombin addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1741870 | Down regulation of TrxR1 expression in human MDA-MB-231 cells at 1.8 uM measured after 72 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Oct-15, Volume: 204 | Design and synthesis of benzylidenecyclohexenones as TrxR inhibitors displaying high anticancer activity and inducing ROS, apoptosis, and autophagy. |
AID1433300 | Effect on SAHA-induced DNA damage in p53 null human U937 cells assessed as decrease in Rad51 expression level by measuring ratio of Rad51 to beta-actin level at 2 uM after 24 hrs by Western blot analysis relative to control | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1474917 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1564520 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy. |
AID1551743 | Antifungal activity against Candida parapsilosis ATCC 22019 after 24 hrs by CLSI broth microdilution method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1551739 | Antifungal activity against Candida albicans ATCC 10231 after 24 hrs by CLSI broth microdilution method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1916767 | Cytotoxicity against human colon epithelial cells incubated for 24 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Dual-target inhibitors of indoleamine 2, 3 dioxygenase 1 (Ido1): A promising direction in cancer immunotherapy. |
AID1455387 | Inhibition of TGF-beta1-regulated decrease in cytoplasmic beta-catenin in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455350 | Antiproliferative activity against human HCT116 cells at 8 uM pretreated with GSH for 1 hr measured after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1433253 | Antiproliferative activity against human CMY cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Synthesis and Antileukemic Activities of Piperlongumine and HDAC Inhibitor Hybrids against Acute Myeloid Leukemia Cells. |
AID1474922 | Induction of reactive oxygen species generation in human HCT116 cells at 10 uM after 1 hr by DCFH-DA dye-based fluorescence microscopic analysis | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1276120 | Cytotoxicity against human HT-29 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1474921 | Cytotoxicity against human W138 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1455322 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1459303 | Induction of tubulin depolymerization in human MCF7 cells at 5 to 20 uM after 4 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1459276 | Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 10 uM after 48 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1426172 | Inhibition of GST in human A549 cells at 5 uM after 1.5 hrs by DNs-CV probe based fluorescence microscopic method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy. |
AID1459277 | Cell cycle arrest in human MCF7 cells assessed as G2/M phase accumulation at 5 uM after 24 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1551757 | Selectivity index, ratio of CC50 for BHK21 cells to IC50 for Candida krusei ATCC 6258 | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1426166 | Inhibition of equine liver GST assessed as decrease in conjugation of CDNB to GSH preincubated with GSH for 30 mins followed by CDNB addition measured for 3 mins | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Developing piperlongumine-directed glutathione S-transferase inhibitors by an electrophilicity-based strategy. |
AID1276121 | Cytotoxicity against human GBM10 cells assessed as cell viability after 72 hrs by resazurin reduction assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Design and synthesis of a C7-aryl piperlongumine derivative with potent antimicrotubule and mutant p53-reactivating properties. |
AID1459265 | Cell cycle arrest in human MCF7 cells assessed as G0/G1 phase accumulation at 10 uM after 24 hrs by propidium iodide staining based flow cytometry | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1430074 | Intrinsic solubility of the compound | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1551750 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of PAF-induced platelet aggregation at 300 uM preincubated for 3 mins followed by PAF addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1551744 | Antibacterial activity against Staphylococcus aureus ATCC 6538 after 24 hrs by CLSI broth microdilution method | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1158952 | Cytotoxicity against human Hep3B cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design, synthesis and biological activity of piperlongumine derivatives as selective anticancer agents. |
AID1377682 | Antiproliferative activity against human K562 cells at 10 uM after 72 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Synthesis and evaluation of N-heteroaromatic ring-based analogs of piperlongumine as potent anticancer agents. |
AID1455334 | Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455319 | Aqueous solubility of compound by HPLC analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455369 | Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as loss of body weight at 4 mg/kg, ip administered thrice a week for 6 consecutive weeks | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1393007 | Growth inhibition of human LNCAP cells after 24 to 48 hrs by WST-1 assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID336832 | Cytotoxicity against mouse P388 cells after 3 days by MTT assay | | | |
AID1206057 | Reduction in total GSH level in human A549 cells at 10 uM after 4 hrs by luminescence assay | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Identification of Novel ROS Inducers: Quinone Derivatives Tethered to Long Hydrocarbon Chains. |
AID1455337 | AUC (0 to infinity) in Sprague-Dawley rat at 20 mg/kg, iv after 4 hrs by LC-MS/MS analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1589250 | Inhibition of MAPK/NFkappaB in ICR mouse RAW264.7 cells assessed as reduction in LPS-induced TNFalpha production at 10 uM pretreated for 0.5 hrs followed by LPS challenge and measured after 24 hrs by ELISA relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI). |
AID1392951 | Effect on total STAT3 protein level in human DU145 cells assessed as ratio of STAT3 protein level to GAPDH protein level at 10 uM after 24 hrs by Western blot analysis (Rvb = 1 No_unit) | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Piperlongumine derivative, CG-06, inhibits STAT3 activity by direct binding to STAT3 and regulating the reactive oxygen species in DU145 prostate carcinoma cells. |
AID1551763 | Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation at 150 uM preincubated for 3 mins followed by arachidonic acid addition measured after 10 mins relative to control | 2019 | European journal of medicinal chemistry, Jul-01, Volume: 173 | Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives. |
AID1455396 | Toxicity in BALB/c nude mouse xenografted with human HCT116 cells assessed as mortality at 4 mg/kg, ip administered thrice a week for 6 consecutive weeks | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1474918 | Antiproliferative activity against human SKHEP1 cells after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11
| Novel non-trimethoxylphenyl piperlongumine derivatives selectively kill cancer cells. |
AID1455383 | Inhibition of TGF-beta1-induced AKT phosphorylation in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1396585 | Senolytic activity against ionizing radiation induced human WI38 senescent cells assessed as reduction in cell viability by propidium iodide staining based flow cytometry | 2018 | Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
| Senolytic activity of piperlongumine analogues: Synthesis and biological evaluation. |
AID1459267 | Antiproliferative activity in human MCF7 cells assessed as cell viability after 48 hrs by alamarBlue assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents. |
AID1173276 | Cytotoxicity against mouse RAW264.7 cells assessed as cell proliferation at 1 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents. |
AID1455326 | Antiproliferative activity against human HCT116 cells after 72 hrs in presence of ligustrazine by MTT assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1455365 | Antiinvasive activity in human HCT116 cells assessed as inhibition of TGF-beta1-induced cell invasion at 50 nM after 48 hrs by crystal violet staining-based assay | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID336830 | Cytotoxicity against human HT-29 cells after 6 days by MTT assay | | | |
AID1677582 | Activation of p38 phosphorylation in human BEL-7402/5-FU cells at 2 uM incubated for 72 hrs by Western blot analysis | | | |
AID1455378 | Inhibition of TGF-beta1-induced increase in expression levels of MMP-9 protein in human HCT116 cells at 50 nM after 48 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
| Novel Ligustrazine-Based Analogs of Piperlongumine Potently Suppress Proliferation and Metastasis of Colorectal Cancer Cells in Vitro and in Vivo. |
AID1430076 | Antitumor activity in human A549 cells xenografted in athymic nude mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered every other day for 21 days | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| Identification of novel ROS inducer by merging the fragments of piperlongumine and dicoumarol. |
AID1589254 | Cytotoxicity against ICR mouse RAW264.7 cells assessed as effect on cell proliferation at 10 uM after 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Design and synthesis novel di-carbonyl analogs of curcumin (DACs) act as potent anti-inflammatory agents against LPS-induced acute lung injury (ALI). |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6
| A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | | | |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |