期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 13, 页码 4606-4614出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.05.034
关键词
Pyrazole derivatives; Thiourea; EGFR; Inhibitors; Anticancer
资金
- National Natural Science Foundation of China [30772627]
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 IC50 of 0.07 mu M, 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 IC50 of 0.08 mu M. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. (C) 2010 Elsevier Ltd. All rights reserved.
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