2. Academic Validation
  3. Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides

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.
Nicholas A Clanton 1,  Shayne D Hastings 2,  Griffin B Foultz 1,  Julie A Contreras 1,  Samantha S Yee 2,  Hadi D Arman 1,  April L Risinger 2 2,  Doug E Frantz 1
Affiliations

Affiliations

  • 1 Department of Chemistry, The University of Texas at San Antonio, San Antonio, Texas 78249, United States.
  • 2 Department of Pharmacology and Mays Cancer Center, University of Texas Health Science Center at San Antonio, San Antonio, Texas 78229-3900, United States.
PMID: 33335677 DOI: 10.1021/acsmedchemlett.0c00534
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.

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