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

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2017 Nov 17

PMID 29144401

Citations 2

Authors

Lin Tang

Tao Peng

Gang Wang

Xiaoxue Wen

Yunbo Sun

Shouguo Zhang

Shuchen Liu

Lin Wang

Affiliations

Soon will be listed here.

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, ()-3-(((4-bromobenzyl)sulfinyl)methylene)indolin-2-one () and ()-3-((benzylsulfinyl)methylene)-5-bromoindolin-2-one () were found to be effective tyrosine kinase inhibitors (IC = 1.34 and 2.69 μM, respectively) in addition to having noteworthy antitumor potential (the average IC value of or was less than 40 μM). This class of novel derivatives has promising potential for further development as anticancer agents.

Citing Articles

Synthesis and antitumor effects of novel benzyl naphthyl sulfoxide/sulfone derivatives derived from Rigosertib.

Tang L, Chen T, Yang H, Wen X, Sun Y, Liu S RSC Adv. 2022; 11(59):37462-37471.

PMID: 35496445 PMC: 9043816. DOI: 10.1039/d1ra05226h.

Design, Synthesis and Preliminary Biological Evaluation of Benzylsulfone Coumarin Derivatives as Anti-Cancer Agents.

Wang T, Peng T, Wen X, Wang G, Sun Y, Liu S Molecules. 2019; 24(22).

PMID: 31703373 PMC: 6891324. DOI: 10.3390/molecules24224034.

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