Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides

ACS Med Chem Lett. 2020 Nov 20;11(12):2534-2543. doi: 10.1021/acsmedchemlett.0c00534. eCollection 2020 Dec 10.


Natural products have served as inspirational scaffolds for the design and synthesis of novel antineoplastic agents. Here we present our preliminary efforts on the synthesis and biological evaluation of a new class of electrophilic steroids inspired by the naturally occurring taccalonolides. We demonstrate that these simplified analogs exhibit highly persistent antiproliferative properties similar to the taccalonolides and retain activity against resistant cancer cell lines that warrants further preclinical development.