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Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides.

ABSTRACT: 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.

SUBMITTER: Clanton NA

PROVIDER: S-EPMC7734803 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature

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Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides.

Clanton Nicholas A NA Hastings Shayne D SD Foultz Griffin B GB Contreras Julie A JA Yee Samantha S SS Arman Hadi D HD Risinger April L AL Frantz Doug E DE

ACS medicinal chemistry letters 20201120 12

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 ...[more]

PMID: 33335677

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