One-Pot Synthesis and Biological Evaluation of Arylpropenone Aminochalcone Conjugates as Potential Apoptotic Inducers

摘要

A facile single pot strategy was developed to synthesize a library of 17 arylpropenone aminochalcone conjugates involving two consecutive reactions, namely Michael addition and Claisen-Schmidt condensation. These conjugates were screened for their in vitro anti-proliferative potential against selected human cancer cell lines such as breast (MCF-7 and MDA-MB231), pancreatic (PANC-1) and colorectal (CaCO2) adenocarcino-ma cells. Among them, the conjugates 6 l and 6p exhibited good to moderate cytotoxicity with IC50 values ranging from 6.7 mu M and 9.8 mu M, respectively, against MCF-7. Furthermore, these conjugates were found to exhibit G0/ G1 cell cycle arrest. Moreover, Annexin-FITC assay revealed that they induced apoptosis in a dose-dependent manner which probably is responsible for their Cytotoxicity