期刊
MOLECULES
卷 22, 期 11, 页码 -出版社
MDPI
DOI: 10.3390/molecules22111979
关键词
sulfoxide; 2-indolinone derivatives; tyrosine kinase inhibitor; anticancer
资金
- National Natural Science Foundation of China [81273431]
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 mu M, respectively) in addition to having noteworthy antitumor potential (the average IC50 value of 6j or 6o was less than 40 mu M). This class of novel derivatives has promising potential for further development as anticancer agents.
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