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

Steroids
Alexander M ScherbakovValerii Z Shirinian

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.

Citations

Jul 15, 2020·Organic & Biomolecular Chemistry·Sadhanendu SamantaAlakananda Hajra
Aug 6, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Svetlana K VorontsovaValerii Z Shirinian
Jan 14, 2021·Organic & Biomolecular Chemistry·Susana M M LopesTeresa M V D Pinho E Melo

❮ Previous
Next ❯

Related Concepts

Related Feeds

Breast Cancer: Therapeutic Approaches

Several different therapeutic approaches are used to treat breast cancer. These include chemotherapy, hormonal therapy, targeted therapy, and Immunotherapy. Discover the latest research on breast cancer therapeutic approaches here.