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Design, Synthesis and Preliminary Biological Evaluation of Novel Benzyl Sulfoxide 2-Indolinone Derivatives as Anticancer Agents.

ABSTRACT: In this work, a series of novel benzyl sulfoxide 2-indolinone derivatives was designed and synthesized as potent anticancer agents. Tyrosine kinase inhibitory activity assay indicated that most of the compounds showed significant activity. The in vitro antiproliferative activity of these compounds was further investigated against five human cancer cell lines (HeLa, HepG2, MCF-7, SCC-15, and A549). Several compounds exhibited evident activities. Among them, (Z)-3-(((4-bromobenzyl)sulfinyl)methylene)indolin-2-one (6j) and (Z)-3-((benzylsulfinyl)methylene)-5-bromoindolin-2-one (6o) were found to be effective tyrosine kinase inhibitors (IC50 = 1.34 and 2.69 ?M, respectively) in addition to having noteworthy antitumor potential (the average IC50 value of 6j or 6o was less than 40 ?M). This class of novel derivatives has promising potential for further development as anticancer agents.

SUBMITTER: Tang L 

PROVIDER: S-EPMC6150246 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature

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Design, Synthesis and Preliminary Biological Evaluation of Novel Benzyl Sulfoxide 2-Indolinone Derivatives as Anticancer Agents.

Tang Lin L   Peng Tao T   Wang Gang G   Wen Xiaoxue X   Sun Yunbo Y   Zhang Shouguo S   Liu Shuchen S   Wang Lin L  

Molecules (Basel, Switzerland) 20171116 11

In this work, a series of novel benzyl sulfoxide 2-indolinone derivatives was designed and synthesized as potent anticancer agents. Tyrosine kinase inhibitory activity assay indicated that most of the compounds showed significant activity. The in vitro antiproliferative activity of these compounds was further investigated against five human cancer cell lines (HeLa, HepG2, MCF-7, SCC-15, and A549). Several compounds exhibited evident activities. Among them, (<i>Z</i>)-3-(((4-bromobenzyl)sulfinyl)  ...[more]

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