1283077-23-5Relevant academic research and scientific papers
Design, synthesis and preliminary biological evaluation of novel benzyl sulfoxide 2-indolinone derivatives as anticancer agents
Tang, Lin,Peng, Tao,Wang, Gang,Wen, Xiaoxue,Sun, Yunbo,Zhang, Shouguo,Liu, Shuchen,Wang, Lin
supporting information, (2017/12/05)
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.
Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials
Praveen Kumar,Gut, Jiri,Guedes, Rita C.,Rosenthal, Philip J.,Santos, Maria M.M.,Moreira, Rui
experimental part, p. 927 - 933 (2011/04/16)
The design, synthesis and evaluation of 3-methylene-substituted indolinones as falcipain inhibitors and antiplasmodial agents are described. These compounds react readily with thiols via an addition-elimination mechanism, indicating their potential as cys
