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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / chemistry
-
Antineoplastic Agents / pharmacology*
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
Chemistry Techniques, Synthetic
-
Dose-Response Relationship, Drug
-
Drug Screening Assays, Antitumor
-
ErbB Receptors / antagonists & inhibitors*
-
ErbB Receptors / metabolism
-
Humans
-
Models, Molecular
-
Molecular Structure
-
Protein Kinase Inhibitors / chemical synthesis*
-
Protein Kinase Inhibitors / chemistry
-
Protein Kinase Inhibitors / pharmacology*
-
Pyrazoles / chemical synthesis
-
Pyrazoles / chemistry
-
Pyrazoles / pharmacology*
-
Stereoisomerism
-
Structure-Activity Relationship
-
Thiazoles / chemical synthesis
-
Thiazoles / chemistry
-
Thiazoles / pharmacology*
Substances
-
Antineoplastic Agents
-
Protein Kinase Inhibitors
-
Pyrazoles
-
Thiazoles
-
ErbB Receptors