Acta Pharmaceutica Sinica 2011;46(11):1338-1343

Synthesis and biological evaluation of 3-aromatic Shiff base-5-fluoroindol-2-one derivatives.

Zheng FANG 1 ; Zhao YANG ; Jia-feng XU ; Yong-lu WANG ; Zhi-xiang WANG ; Ping WEI

Affiliations

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Country

China

Language

Chinese

Abstract

Based on the structure of 5-fluoroindol-2-one and fragments from thirteen multi-target tyrosine kinase inhibitors which have been marketed or in the phase of clinical research, eleven 3-aromatic Shiff base-5-fluoroindol-2-one derivatives were designed and synthesized. Their structures were identified by 1H NMR, MS and elemental analysis. In vitro antitumor bioactivities evaluation was done by MTT method. It was shown that most of synthesized compounds had antitumor activities and compounds 1b, 1g, 1i and 1h were better than or equal to the antitumor activity of positive control.