Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides

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

doi:10.1021/acsmedchemlett.0c00534

Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides

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

Department of Pharmacology

Research output: Contribution to journal › Article › peer-review

3 Scopus citations

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.

Original language	English (US)
Pages (from-to)	2534-2543
Number of pages	10
Journal	ACS Medicinal Chemistry Letters
Volume	11
Issue number	12
DOIs	https://doi.org/10.1021/acsmedchemlett.0c00534
State	Published - Dec 10 2020

Keywords

natural products
ovarian cancer
steroids
triple negative breast cancer

ASJC Scopus subject areas

Drug Discovery
Biochemistry
Organic Chemistry

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10.1021/acsmedchemlett.0c00534

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title = "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.",

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AU - Foultz, Griffin B.

AU - Contreras, Julie A.

AU - Yee, Samantha S.

AU - Arman, Hadi D.

AU - Risinger, April L.

AU - Frantz, Doug E.

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PY - 2020/12/10

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N2 - 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.

AB - 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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KW - steroids

KW - triple negative breast cancer

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Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides

Abstract

Keywords

ASJC Scopus subject areas

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