Synthesis and biological evaluation of sulphonyl derivatives of naturally occurring chromone alkaloid of rohitukine as anticancer agents

Abstract

The present study deals with isolation of active constituent, rohitukine from the stem bark of Dysoxylum binectariferum, and synthesis of a series of its new sulphonyl derivatives aiming to enhance its therapeutic efficacy. Rohitukine has been isolated with more than 95% purity and ten new semisynthetic analogs have been prepared using different sulphonyl chlorides. These derivatives were evaluated for anticancer activity against MCF-7 (ER +ve) and MDA-MB-231 (ER -ve) breast cancer cell lines. Compounds K6, K8 and K10 showed significant activity against breast cancer cell lines at a concentration of 17.5 µM, 17 µM and 19 µM in MCF-7 and 20 µM, 9.8 µM and 28.5 µM in MDA-MB-231 respectively. These compounds induced significant apoptosis in MCF-cell line. Further work may enhance the anticancer activity.