Discovery and potency optimization of 2-amino-5-arylmethyl-1,3-thiazole derivatives as potential therapeutic agents for prostate cancer Article

Krasavin, M, Karapetian, R, Konstantinov, I et al. (2009). Discovery and potency optimization of 2-amino-5-arylmethyl-1,3-thiazole derivatives as potential therapeutic agents for prostate cancer . ARCHIV DER PHARMAZIE, 342(7), 420-427. 10.1002/ardp.200800201

cited authors

  • Krasavin, M; Karapetian, R; Konstantinov, I; Gezentsvey, Y; Bukhryakov, K; Godovykh, E; Soldatkina, O; Lavrovsky, Y; Sosnov, AV; Gakh, AA

authors

abstract

  • A new chemical series was identified via high-throughput screening as having antiproliferative activity on DU-145 human prostate carcinoma cell line (hit compound potency - 2.9 μM). Medicinal chemistry optimization of two peripheral diversity vectors of the hit molecule, independently, led to SAR generalizations and identification of the 'best' moieties. The latter were merged in a single compound that exhibited an over 100-fold better potency than the hit compound. For the most potent compounds it was confirmed that the observed antiproliferative potency was not associated with the compounds' non-specific cytotoxicity. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

publication date

  • July 1, 2009

published in

Digital Object Identifier (DOI)

start page

  • 420

end page

  • 427

volume

  • 342

issue

  • 7