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SpringerOpen, Chemistry Central Journal, 1(4), 2010

DOI: 10.1186/1752-153x-4-4

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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

Journal article published in 2010 by Mikhail Krasavin ORCID, Konstantin A. Rufanov, Andrey V. Sosnov, Ruben Karapetian, Elena Godovykh, Olga Soldatkina, Yan Lavrovsky, Andrei A. Gakh
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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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 microM). 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.