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Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series Full article

Journal Steroids
ISSN: 1878-5867 , E-ISSN: 0039-128X
Output data Year: 2018, Volume: 138, Pages: 91-101 Pages count : 11 DOI: 10.1016/j.steroids.2018.06.013
Authors Scherbakov Alexander M. 1 , Zavarzin Igor V. 2 , Vorontsova Svetlana K. 2 , Hajra Alakananda 3 , Andreeva Olga E. 1 , Yadykov Anton V. 2 , Levina Inna S. 2 , Volkova Yulia A. 2 , Shirinian Valerii Z. 2
Affiliations
1 N.N. Blokhin National Medical Research Center of Oncology, Kashirskoye shosse 24, 115478 Moscow, Russia
2 N. D. Zelinsky-Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky Prosp. 47, 119991 Moscow, Russia
3 Department of Chemistry, Visva-Bharati (A Central University), Santiniketan-, India

Abstract: Novel benzylidenes (chalcones) of the 16-dehydroprogesterone series have been characterized and their antitumor activity against two breast cancer cell lines was evaluated. Benzylidenes exhibit significant antiproliferative effect on cells and inhibit cell growth in hormone-dependent MCF-7 and hormone-independent MDA-MB-231 breast cancer cell lines. Compound 3d exhibits the highest activity against two breast cancer cell lines, with the IC50 value of about 2 µM. Compounds 3e,m,n display considerable selectivity for hormone-dependent breast cancer cells, with the IC50 value lower than 6 µM. Moreover, these steroidal benzylidenes regulate ERα signaling and reveal p53-independent mechanism of pro-apoptotic action in MCF-7 cells. The new class of antitumor compounds holds promise as the basis for the design of agents for cancer therapy.
Cite: Scherbakov A.M. , Zavarzin I.V. , Vorontsova S.K. , Hajra A. , Andreeva O.E. , Yadykov A.V. , Levina I.S. , Volkova Y.A. , Shirinian V.Z.
Synthesis and evaluation of the antiproliferative activity of benzylidenes of 16-dehydroprogesterone series
Steroids. 2018. V.138. P.91-101. DOI: 10.1016/j.steroids.2018.06.013 WOS Scopus OpenAlex
Identifiers:
≡ Web of science: WOS:000444932400013
≡ Scopus: 2-s2.0-85050140282
≡ OpenAlex: W2828711158
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