Optimization of the anti-cancer activity of the phosphatidylinositol-3 kinase pathway inhibitor PITENIN-1: switching thiourea with 1,2,3-triazole

Kommagalla, Yadagiri ; Cornea, Sinziana ; Riehle, Robert ; Torchilin, Vladimir ; Degterev, Alexei ; Ramana, Chepuri V. (2014) Optimization of the anti-cancer activity of the phosphatidylinositol-3 kinase pathway inhibitor PITENIN-1: switching thiourea with 1,2,3-triazole MedChemComm, 5 (9). pp. 1359-1363. ISSN 2040-2503

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Official URL: http://pubs.rsc.org/en/Content/ArticleLanding/2014...

Related URL: http://dx.doi.org/10.1039/C4MD00109E

Abstract

We previously reported encouraging in vitro and in vivo anti-cancer activity of N-((3-chloro-2-hydroxy-5-nitrophenyl)carbamothioyl)benzamide (termed PITENIN-1). In the current work, we describe the structure–activity relationship study of the PIT-1 series, based on the replacement of a central thiourea unit with 1,2,3-triazole, which leads to increased liver microsomal stability, drug likeness and toxicity towards cancer cells.

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