Cytotoxic activity and molecular modeling of progestins, pregna-D′-pentaranes
- Autores: Scherbakov A.M.1, Levina I.S.2, Kulikova L.E.2, Fedyushkina I.V.3,4, Skvortsov V.S.3, Veselovsky A.V.3, Kuznetsov Y.V.2, Zavarzin I.V.2
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Afiliações:
- Blokhin Russian Cancer Research Centre (RCRC)
- Zelinsky Institute of Organic Chemistry Russian Academy of Sciences
- Institute of Biomedical Chemistry
- Institute of Physical-Chemical Medicine
- Edição: Volume 10, Nº 4 (2016)
- Páginas: 341-345
- Seção: Article
- URL: https://journals.rcsi.science/1990-7508/article/view/197558
- DOI: https://doi.org/10.1134/S1990750816040077
- ID: 197558
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Resumo
The cytotoxic activity of synthetic progestins (pregna-D′-pentaranes II–V), full agonists of the progesterone receptor (PR), has been investigated towards PR-positive and PR-negative cells of human breast carcinoma. These compounds were more active in PR-positive MCF-7 cells than in PR-negative MDA-MB-453 cells. The tested compounds did not demonstrate cytotoxic effects towards normal epithelial MDCK cells. Molecular modeling of studied steroids with PR showed that all progestins with close energy values could bind to the ligand binding domain (LBD) of PR and the magnitude of the energy exceeded the value estimated for the progesterone molecule. Thus, the studied progestins are active towards different molecular subtypes of breast cancer and represent a promising class of chemical compounds for oncology.
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Sobre autores
A. Scherbakov
Blokhin Russian Cancer Research Centre (RCRC)
Autor responsável pela correspondência
Email: alex.scherbakov@gmail.com
Rússia, Kashirskoe sh. 24, Moscow, 115478
I. Levina
Zelinsky Institute of Organic Chemistry Russian Academy of Sciences
Autor responsável pela correspondência
Email: li@ioc.ac.ru
Rússia, Leninskii pr. 47, Moscow, 119991
L. Kulikova
Zelinsky Institute of Organic Chemistry Russian Academy of Sciences
Email: li@ioc.ac.ru
Rússia, Leninskii pr. 47, Moscow, 119991
I. Fedyushkina
Institute of Biomedical Chemistry; Institute of Physical-Chemical Medicine
Email: li@ioc.ac.ru
Rússia, ul. Pogodinskaya 10, Moscow, 119121; ul. Malaya Pirogovskaya 1a, Moscow, 119435
V. Skvortsov
Institute of Biomedical Chemistry
Email: li@ioc.ac.ru
Rússia, ul. Pogodinskaya 10, Moscow, 119121
A. Veselovsky
Institute of Biomedical Chemistry
Email: li@ioc.ac.ru
Rússia, ul. Pogodinskaya 10, Moscow, 119121
Yu. Kuznetsov
Zelinsky Institute of Organic Chemistry Russian Academy of Sciences
Email: li@ioc.ac.ru
Rússia, Leninskii pr. 47, Moscow, 119991
I. Zavarzin
Zelinsky Institute of Organic Chemistry Russian Academy of Sciences
Email: li@ioc.ac.ru
Rússia, Leninskii pr. 47, Moscow, 119991
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