Kommagalla Yadagiri, Cornea Sinziana, Riehle Robert, Torchilin Vladimir, Degterev Alexei, Ramana Chepuri V
Division of Organic Chemistry, CSIR-National Chemical Laboratory, Pune, India 411008.
Department of Developmental, Molecular and Chemical Biology, Tufts University, 136 Harrison Avenue, Boston, MA 02111.
Medchemcomm. 2014 Sep;5(9):1359-1363. doi: 10.1039/C4MD00109E.
We previously reported encouraging and anti-cancer activity of -((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.
我们之前报道了-((3-氯-2-羟基-5-硝基苯基)氨基甲硫酰基)苯甲酰胺(称为PITENIN-1)令人鼓舞的抗癌活性。在当前工作中,我们描述了PIT-1系列的构效关系研究,该研究基于用1,2,3-三唑取代中心硫脲单元,这导致肝微粒体稳定性增加、药物相似性以及对癌细胞的毒性增强。