Novel substituted 5-arylidene-1, 3-thiazolidin-4-one analogues: Synthesis, optimization, anticancer screening and docking studies

Abstract

We have developed novel series of 5-arylidene-1, 3-thiazolidin-4-one analogues using diethylamine as catalyst. Diethylamine was found suitable in synthesizing variety of title compounds in 62-85% yield. In-vitro anticancer activity of synthesized analogues was evaluated using human breast (MCF7), lung (Hop62) and hepatic (HepG2) cell lines using SRB assay. Amongst the synthesized compounds 9b, 9e, 9f are excellent in inhibiting growth of cancer cell lines with GI50 value <10μg/ml in comparison with Adriamycin standard. We have also performed docking studies using SHP2 in complex with inhibitor (PDB ID: 2Shp) but results were non-supportive, very weak. We found no correlation between anticancer studies and docking studies.