Anti-proliferative, structure–activity relationship of pyridinylchalcones and chromanones

A series of pyridinylchalcones 3a – q , chromanones 4a – q were prepared and screened for their in vitro anti-proliferative activity against four human cancer cell lines viz ., cervical (HeLa), lung adenocarcinoma (A549), prostate (DU-145) and breast (MDA-MB-231). Pyridinylchalcones 3a-q and chromanones 4a-q exhibited IC 50 values in the range of 5.9–289 µM. Compound 3e exhibited an IC 50 of 5.9 µM and also increased caspase-3 activity to ~ 2.7-fold at 10 µM concentration in HeLa cell line. Cell cycle analysis further confirmed the apoptotic effects of 3e due to a substantial increase in cells arrested at sub-G1 phase of cell cycle. Further, the loss of mitochondrial membrane potential in 3e treated cells indicates that the intrinsic pathway of apoptosis might be responsible in 3e induced apoptosis. Graphical Abstract Pyridinylchalcones, chromanones were screened for their in vitro anti-proliferative activity against four human cancer cell lines by the standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay method. Pyridinylchalcones and chromanones exhibited IC 50 values in the range of 5.9–289 µM. Compound 3e exhibited an IC 50 of 5.9 µM and also increased caspase-3 activity to ~2.7-fold at 10 µM concentration in HeLa cell line