1234016-38-6Relevant articles and documents
Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives as EGFR TK inhibitors and potential anticancer agents
Lv, Peng-Cheng,Li, Dong-Dong,Li, Qing-Shan,Lu, Xiang,Xiao, Zhu-Ping,Zhu, Hai-Liang
, p. 5374 - 5377 (2011/10/12)
Fourty-two thiazolyl-pyrazoline derivatives were synthesized to screen for their EGFR kinase inhibitory activity. Compound 4-(4-chlorophenyl)-2-(3-(3,4- dimethylphenyl)-5-p-tolyl-4,5-dihydro-1H-pyrazol-1-yl)thiazole (11) displayed the most potent EGFR TK inhibitory activity with IC50 of 0.06 μM, which was comparable to the positive control. Molecular docking results indicated that compound 11 was nicely bound to the EGFR kinase. Compound 11 also showed significant antiproliferative activity against MCF-7 with IC 50 of 0.07 μM, which would be a potential anticancer agent.