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Molecules 2016, 21(8), 1012; doi:10.3390/molecules21081012

Design, Synthesis and Biological Evaluation of Benzohydrazide Derivatives Containing Dihydropyrazoles as Potential EGFR Kinase Inhibitors

1
College of Biology and Food Engineering, Suzhou University, Suzhou 234000, China
2
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, China
*
Authors to whom correspondence should be addressed.
Academic Editor: James W. Leahy
Received: 2 June 2016 / Revised: 12 July 2016 / Accepted: 29 July 2016 / Published: 3 August 2016
(This article belongs to the Special Issue Kinase Inhibitor Chemistry)
View Full-Text   |   Download PDF [3933 KB, uploaded 3 August 2016]   |  

Abstract

A series of novel benzohydrazide derivatives containing dihydropyrazoles have been synthesized as potential epidermal growth factor receptor (EGFR) kinase inhibitors and their biological activities as potential antiproliferative agents have been evaluated. Among these compounds, compound H20 exhibited the most potent antiproliferative activity against four cancer cell line variants (A549, MCF-7, HeLa, HepG2) with IC50 values of 0.46, 0.29, 0.15 and 0.21 μM respectively, which showed the most potent EGFR inhibition activities (IC50 = 0.08 μM for EGFR). Molecular modeling simulation studies were performed in order to predict the biological activity and activity relationship (SAR) of these benzohydrazide derivatives. These results suggested that compound H20 may be a promising anticancer agent. View Full-Text
Keywords: benzohydrazide derivatives; EGFR inhibitor; antiproliferative activity; cytotoxicity; molecular docking benzohydrazide derivatives; EGFR inhibitor; antiproliferative activity; cytotoxicity; molecular docking
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Wang, H.-C.; Yan, X.-Q.; Yan, T.-L.; Li, H.-X.; Wang, Z.-C.; Zhu, H.-L. Design, Synthesis and Biological Evaluation of Benzohydrazide Derivatives Containing Dihydropyrazoles as Potential EGFR Kinase Inhibitors. Molecules 2016, 21, 1012.

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