Synthesis and primary cytotoxicity evaluation of new 5-benzylidene-2,4-thiazolidinedione derivatives

In the present work, ten novel derivatives (3a–3j) of 5-benzylidene-2,4-thiazolidinediones were synthesized and their structures were determined by analytical and spectral (FTIR, 1H NMR, 13C NMR) methods. The newly synthesized compounds were evaluated for their antiproliferative activity at Tata Memorial’s Advanced Center for Treatment, Research and Education in Cancer (ACTREC), India, in a panel of 7 cancer cell lines using four concentrations at 10-fold dilutions. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. Though the compounds showed varying degrees of cytotoxicity in the tested cell lines, most marked effect was observed by compound 3e in MCF7 (breast cancer), K562 (leukemia) and GURAV (nasopharyngeal cancer) cell lines with log10 GI50 values of −6.7, −6.72 and −6.73 respectively.

Graphical abstractIn this communication, a series of ten (3a–3j) novel 5-benzylidene-2,4-thiazolidinedione derivatives were synthesized and evaluated in vitro against different human cancer cell linesFigure optionsDownload full-size imageDownload as PowerPoint slide