29805-21-8Relevant articles and documents
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.
, p. 1359 - 1363 (2014)
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.