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

Producción científica: Article › revisión exhaustiva

4 Citas (Scopus)

Resumen

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.

Idioma original	English (US)
Páginas (desde-hasta)	2534-2543
Número de páginas	10
Publicación	ACS Medicinal Chemistry Letters
Volumen	11
N.º	12
DOI	https://doi.org/10.1021/acsmedchemlett.0c00534
Estado	Published - dic 10 2020

ASJC Scopus subject areas

Drug Discovery
Biochemistry
Organic Chemistry

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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 - ovarian cancer

KW - steroids

KW - triple negative breast cancer

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Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides

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