Cytotoxic activity and molecular modeling of progestins, pregna-D′-pentaranes


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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.

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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