Cytotoxic activity and molecular modeling of progestins - pregna-D'-pentarans

Scherbakov A.M.1 , Levina I.S.2, Kulikova L.E.2, Fedyushkina I.V.3, Skvortsov V.S.4, Veselovsky A.V.4, Kuznetsov Y.V.2, Zavarzin I.V.2

1. Blokhin Cancer Research Centre, Moscow, Russia
2. Zelinsky Institute of Organic Chemistry Russian Academy of Sciences, Moscow, Russia
3. Institute of Biomedical Chemistry, Moscow, Russia; SRI of Physical-Chemical Medicine Federal Medical and Biological Agency, Moscow, Russia
4. Institute of Biomedical Chemistry, Moscow, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20166203290      PubMed Id: 27420621
Year: 2016  Volume: 62  Issue: 3  Pages: 290-294
The cytotoxic activity of synthetic progestins (pregna-D'-pentaranes) II-V full agonists of the progesterone receptor (PR) for PR-positive and PR-negative cells of human breast carcinoma was studied. These compounds were more active in the PR-positive MCF-7 cells than in the PR-negative MDA-MB-453 cells. Cytotoxic effects of tested compounds against normal epithelial MDCK cells were not found. Molecular modeling of studied steroids with PR showed that all progestins with close energy values can bind to the ligand binding domain (LBD) of PR and the magnitude of the energy exceeds the value estimated for the progesterone molecule. Thus, the studied progestins are active against different molecular subtypes of breast cancer and represent a promising class of chemical compounds for oncology.
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Keywords: pentaranes, progesterone receptor, cytotoxic activity, molecular modeling

Scherbakov, A. M., Levina, I. S., Kulikova, L. E., Fedyushkina, I. V., Skvortsov, V. S., Veselovsky, A. V., Kuznetsov, Y. V., Zavarzin, I. V. (2016). Cytotoxic activity and molecular modeling of progestins - pregna-D'-pentarans. Biomeditsinskaya Khimiya, 62(3), 290-294.
This paper is also available as the English translation: 10.1134/S1990750816040077
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