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Discovery and SAR exploration of N-aryl-N-(3-aryl-1,2,4-oxadiazol-5-yl)amines as potential therapeutic agents for prostate cancer

Author(s): Krasavin Mikhail | Rufanov Konstantin | Sosnov Andrey | Karapetian Ruben | Godovykh Elena | Soldatkina Olga | Lavrovsky Yan | Gakh Andrei

Journal: Chemistry Central Journal
ISSN 1752-153X

Volume: 4;
Issue: 1;
Start page: 4;
Date: 2010;
Original page

Abstract A new chemical series of antiproliferative compounds was identified via high-throughput screening on DU-145 human prostate carcinoma cell line (hit compound potency - 5.7 μM). Exploration of the two peripheral diversity vectors of the hit molecule in a hit-targeted library and testing of the resulting compounds led to SAR generalizations and identification of the 'best' pharmacophoric moieties. The latter were merged in a single compound that exhibited a 200-fold better potency than the original hit compound. Specific cancer cell cytotoxicity was confirmed for the most potent compounds.
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