Syntheses of conformationally restricted benzopyran based triarylethylenes as growth inhibitors of carcinoma cells

Abstract A series of conformationally restricted benzopyran based triarylethylenes has been synthesized and characterized as potential growth inhibitors of breast carcinoma cells. The synthesized compounds ( 14a–b , 15a and 16a–e ) presented significant growth inhibition of ER+ and ER− breast cancer cells within the range of IC 50 0.55–9.96 µM. Amongst other, 16c showed potent anticancer activity at IC 50 0.95 µM in MCF-7 cells with good selectivity (Selectivity Index 4.47) towards healthy cells. The mechanistic studies for 16c were performed to elucidate possible mode of action which showed 16c elicited anticancer activity through necroptosis process.