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Molecules 2017, 22(11), 1979; doi:10.3390/molecules22111979

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

Beijing Institute of Radiation Medicine, Beijing 100850, China
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Received: 12 October 2017 / Revised: 13 November 2017 / Accepted: 14 November 2017 / Published: 16 November 2017
(This article belongs to the Section Medicinal Chemistry)
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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 μM, respectively) in addition to having noteworthy antitumor potential (the average IC50 value of 6j or 6o was less than 40 μM). This class of novel derivatives has promising potential for further development as anticancer agents. View Full-Text
Keywords: sulfoxide; 2-indolinone derivatives; tyrosine kinase inhibitor; anticancer sulfoxide; 2-indolinone derivatives; tyrosine kinase inhibitor; anticancer
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MDPI and ACS Style

Tang, L.; Peng, T.; Wang, G.; Wen, X.; Sun, Y.; Zhang, S.; Liu, S.; Wang, L. Design, Synthesis and Preliminary Biological Evaluation of Novel Benzyl Sulfoxide 2-Indolinone Derivatives as Anticancer Agents. Molecules 2017, 22, 1979.

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