Abstract:
: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 IC(50) 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.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Lv PC,Li DD,Li QS,Lu X,Xiao ZP,Zhu HLdoi
10.1016/j.bmcl.2011.07.010subject
Has Abstractpub_date
2011-09-15 00:00:00pages
5374-7issue
18eissn
0960-894Xissn
1464-3405pii
S0960-894X(11)00948-6journal_volume
21pub_type
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