n-phenylacrylamide and pyrazole

n-phenylacrylamide has been researched along with pyrazole* in 1 studies

Other Studies

1 other study(ies) available for n-phenylacrylamide and pyrazole

Article	Year
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity. Bioorganic & medicinal chemistry, 2012, Jul-15, Volume: 20, Issue:14 In present study, a series of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives (5a-8d) were designed, synthesized, and evaluated for HDAC inhibition and tumor cell antiproliferation. All of these compounds are reported for the first time, the chemical structures of these compounds were confirmed by means of (1)H NMR, ESI-MS and elemental analyzes. Among the compounds, compound 8c showed the most potent biological activity against HCT116 cancer cell line (IC(50) of 0.42 ± 0.02 μM for HDAC-1 and IC(50)=0.62 ± 0.02 for HCT116). Docking simulation was performed to position compound 8c into the HDAC active site to determine the probable binding model. The results of antiproliferative assay and western-blot demonstrated that compound 8c with potent inhibitory activity in tumor growth inhibition may be a potential anticancer agent against HCT116 cancer cell. Topics: Acrylamides; Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Cell Proliferation; Computer Simulation; Drug Screening Assays, Antitumor; HCT116 Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Protein Structure, Tertiary; Pyrazoles; Structure-Activity Relationship	2012

Article

Year

Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.

Bioorganic & medicinal chemistry, 2012, Jul-15, Volume: 20, Issue:14

In present study, a series of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives (5a-8d) were designed, synthesized, and evaluated for HDAC inhibition and tumor cell antiproliferation. All of these compounds are reported for the first time, the chemical structures of these compounds were confirmed by means of (1)H NMR, ESI-MS and elemental analyzes. Among the compounds, compound 8c showed the most potent biological activity against HCT116 cancer cell line (IC(50) of 0.42 ± 0.02 μM for HDAC-1 and IC(50)=0.62 ± 0.02 for HCT116). Docking simulation was performed to position compound 8c into the HDAC active site to determine the probable binding model. The results of antiproliferative assay and western-blot demonstrated that compound 8c with potent inhibitory activity in tumor growth inhibition may be a potential anticancer agent against HCT116 cancer cell.

Topics: Acrylamides; Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Cell Proliferation; Computer Simulation; Drug Screening Assays, Antitumor; HCT116 Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Protein Structure, Tertiary; Pyrazoles; Structure-Activity Relationship

2012