New Nitrogen-containing Androstane Derivatives Suppressing Prostate Carcinoma Cells Proliferation

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Published: Oct 1, 2024
DOI: https://doi.org/10.18097/BMCRM00241
Keywords:
molecular docking; antiproliferative activity; synthesis of steroid derivatives; CYP17A1 inhibitors; prostate carcinoma cells; nitrogen-containing steroid derivatives

Main Article Content

A.S. Latysheva
Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
A.Yu. Misharin
Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
A.V. Veselovsky
Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
G.E. Morozevich
Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia
R.A. Novikov
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, 32 Vavilov str., Moscow, 119991 Russia
V.A. Zolottsev
Institute of Biomedical Chemistry, 10 Pogodinskaya str., Moscow, 119121 Russia

Abstract

Derivatives of 3β-hydroxyandrost-5,16-diene and 3β-hydroxyandrost-5-ene containing 2-oxazoline, 2-benzoxazole, and 2-benzimidazole substituents at C-17 position were synthesized. Docking of the synthesized compounds into the active site of human CYP17A1 predicted their high affinity for the enzyme. Of the 6 new compounds, 5 suppressed the proliferation of prostate carcinoma cells LNCaP and PC-3, and the activity of the oxazoline and benzimidazole derivatives of androsta-5,16-diene significantly exceeded the activity of the known anticancer agents abiraterone and galeterone.

Article Details

How to Cite
Latysheva, A., Misharin, A., Veselovsky, A., Morozevich, G., Novikov, R., & Zolottsev, V. (2024). New Nitrogen-containing Androstane Derivatives Suppressing Prostate Carcinoma Cells Proliferation. Biomedical Chemistry: Research and Methods, 7(3), e00241. https://doi.org/10.18097/BMCRM00241
Issue
Vol. 7 No. 3 (2024)
Section
EXPERIMENTAL RESEARCH

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