Synthesis and biological evaluation of novel 2-heteroarylimino-1,3-thiazolidin-4-ones as potential anti-tumor agents

European Journal of Medicinal Chemistry
Germain RevelantStéphanie Hesse

Abstract

A series of 35 heteroarylimino-1,3-thiazolidinones with three sites of functionalization were synthesized and their antiproliferative properties were studied. The in vitro screening by MTT assay was performed against five cancer cell lines (human colon cancer cell lines HT29, HCT116 and SW620 and breast cancer cell lines MCF7 and MDA-MB-231). It was observed that N3-substituted thiazolidinones had moderate activities whereas 5-benzylidene thiazolidinones showed promising activities. To investigate the mechanism of action, detailed biological studies of six selected compounds (those presenting the lower mitotic index) were carried out on the human colon cancer HT29 cell line. Cell cycle assay revealed that those compounds induced cell accumulation in G2/M and in subG0/G1 phases of cell cycle. Moreover, dissipation of mitochondria membrane potential was observed as well as redox changes in treated cells.

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Citations

Feb 21, 2016·European Journal of Medicinal Chemistry·Danylo KaminskyyRoman Lesyk
Feb 9, 2016·Chemistry Central Journal·Andreea-Teodora PânzariuCristina Tuchilus
Apr 19, 2016·European Journal of Medicinal Chemistry·Julia SenkivRoman Lesyk
Sep 12, 2016·European Journal of Medicinal Chemistry·Daniel Schuch da SilvaWilson Cunico
Sep 10, 2019·Organic & Biomolecular Chemistry·Abderrahman El BouakherSébastien Comesse
Jul 25, 2019·Scientific Reports·Konrad A SzychowskiJan Gmiński
Mar 25, 2020·Topics in Current Chemistry·Nusrat SahibaShikha Agarwal
Sep 1, 2019·Bioorganic & Medicinal Chemistry·Ravi P SinghCarl J Lovely

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