Optimization of the anti-cancer activity of the phosphatidylinositol-3 kinase pathway inhibitor PITENIN-1: switching thiourea with 1,2,3-triazoleElectronic supplementary information (ESI) available: Synthesis and characterization data and spectra of all the new compounds. See DOI: 10.1039/c4md00109e

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 thio...

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Main Authors: Kommagalla, Yadagiri, Cornea, Sinziana, Riehle, Robert, Torchilin, Vladimir, Degterev, Alexei, Ramana, Chepuri V
Format: Article
Language:English
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Summary: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. Replacement of a central thiourea unit of PITENINs (inhibitors of the phosphatidylinositol-3 kinase (PI3K) signaling pathway) with 1,2,3-triazole, lead to increased liver microsomal stability, drug likeness and toxicity towards cancer cells.
ISSN:2040-2503
2040-2511
DOI:10.1039/c4md00109e