Open AccessSynthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides
Author(s) -
Nicholas A. Clanton,
Shayne D. Hastings,
Griffin B. Foultz,
Julie A. Contreras,
Samantha S. Yee,
Hadi D. Arman,
April L. Risinger,
Doug E. Frantz
Publication year - 2020
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/acsmedchemlett.0c00534
Subject(s) - electrophile , combinatorial chemistry , computational biology , cancer cell lines , chemistry , computer science , biology , cancer , biochemistry , cancer cell , genetics , catalysis
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.