Novel thiazolidines: Synthesis, antiproliferative properties and 2D-QSAR studies.

Bioorg Med Chem

Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA. Electronic address:

Published: October 2019

A series of N-substituted (Z)-2-imino-(5Z)-ylidene thiazolidines/thiazolidin-4-ones were synthesized and their antiproliferative activities against colon (HCT-116) and breast (MCF7) cancer cell lines were evaluated utilizing an MTT growth assay. A 2D-QSAR investigation was conducted to probe and validate the obtained antiproliferative properties for the thiazolidine derivatives. The majority of the thiazolidines exhibit higher potency against a colon cancer cell line relative to the standard reference. The p-halophenylimino p-anisylidene derivatives exhibited the highest anti-proliferative activity against HCT116 relative to control (IC = 8.9-10.0 μM compared to 20.4 μM observed for 5-fluorouracil as positive control). An X-ray study confirmed the Z, Z'-configurations for two examples of the synthesized compounds.

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http://dx.doi.org/10.1016/j.bmc.2019.115047DOI Listing

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