Synthesis and Cytostatic Activity of New Mepregenol 17-Acetate Derivatives with Respect to Hela Cancer Cell Culture

Autor:	N. I. Sheina, Nadezhda I. Fedotcheva, T. A. Fedotcheva, E. D. Sveshnikova, Mikhail N. Sokolov, Konstantin V. Kudryavtsev, N. L. Shimanovskii
Rok vydání:	2020
Předmět:	Pharmacology biology 010405 organic chemistry Chemistry Pharmacology toxicology biology.organism_classification 01 natural sciences 0104 chemical sciences HeLa Comet assay 010404 medicinal & biomolecular chemistry Biochemistry Megestrol acetate Drug Discovery Cancer cell Ic50 values medicine Cytotoxicity medicine.drug
Zdroj:	Pharmaceutical Chemistry Journal. 54:119-125
ISSN:	1573-9031 0091-150X
Popis:	New mepregenol 17-acetate derivatives with potential cytotoxicity were synthesized. Mepregenol 17-acetate 3-acrylate (III) was shown to exhibit potent cytotoxicity although the ester of N-benzylpyrrolidine-3-carboxylic acid (IV) had weaker activity that was comparable with those of megestrol acetate and progesterone. The IC50 values for III, IV, progesterone, and megestrol acetate were 30, 200, 480, and 130 μMwith respect to native HeLa culture and 9.1, 180, 5.6, and 115 μm for an estradiol-stimulated culture of HeLa, respectively. The cytotoxicities of steroids III and IV correlated with their DNA-damaging effect in a DNA comet assay. Thus, III was promising for further research as an antitumor compound with respect to estradiol-dependent tumors.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::0f311518cdc77ef4cf6ea9942e7ac4c1 https://doi.org/10.1007/s11094-020-02167-1 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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