Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents

Compound C5 exhibited the most potent EGFR inhibitory activity with IC 50 of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Besides, compound C5 showed signif...

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Published in:Bioorganic & medicinal chemistry 2010-07, Vol.18 (13), p.4606-4614
Main Authors: Lv, Peng-Cheng, Li, Huan-Qiu, Sun, Juan, Zhou, Yang, Zhu, Hai-Liang
Format: Article
Language:English
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Summary:Compound C5 exhibited the most potent EGFR inhibitory activity with IC 50 of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Besides, compound C5 showed significant antiproliferative activity against MCF-7 with IC 50 of 0.08 μM, which would be a potential anticancer agent. Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been discovered. Some of them exhibited significant EGFR inhibitory activity. Compound 3-(3,4-dimethylphenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide ( C5) displayed the most potent EGFR inhibitory activity with IC 50 of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the pyrazole derivatives own high antiproliferative activity against MCF-7. Compound C5 showed significant antiproliferative activity against MCF-7 with IC 50 of 0.08 μM. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2010.05.034