Design and Synthesis of New Agents for Prostate Cancer Treatment Inspired by Steroidal CYP17 A1 Inhibitors

• DOI: 10.1002/slct.202203393
• Publication Date: 2022-12-02T10:08:33Z
• Authors: Vladimir A. Zolot...; Alexandra S. Laty...; Irina I. Khan; Vadim S. Pokrovsky; Alexander Y. Mish...
• Keywords: Oxazoline

Abstract Steroid derivatives modified with nitrogen containing heterocycles attract attention as anticancer agents for prostate cancer treatment. In this study we have developed a simple and convenient procedure preparation of 17(20)‐21‐norpregnene androst‐16‐ene 2’‐oxazolinyl 2’‐benzoxazolyl derivatives, based on the reaction an appropriately steroidal carboxylic acid 1,2‐amino alcohols or o‐aminophenol. Using method conducted synthesis series new steroid hybrids differing either in structure part, heterocycle (23 compounds total). Some revealed high anti‐proliferative activity carcinoma LNCaP PC‐3 cells, exceeding that well‐known abiraterone galeterone. Oxazoline derivative [17(20)]‐21‐norpregnene potently stimulated apoptosis DU‐145 cells inhibited growth tumors 22Rv1 derived xenograft models direct comparison abiraterone.