Unknown

Dataset Information

0

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

ABSTRACT: We previously reported encouraging in vitro and in vivoanti-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 PIT-1 series, based on the replacement of central thiourea unit with a 1,2,3-triazole, which leads to increased liver microsomal stability, drug likeness and toxicity towards cancer cells.

SUBMITTER: Kommagalla Y 

PROVIDER: S-EPMC4259262 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

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

Kommagalla Yadagiri Y   Cornea Sinziana S   Riehle Robert R   Torchilin Vladimir V   Degterev Alexei A   Ramana Chepuri V CV  

MedChemComm 20140901 9

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