title: 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 encouragingin vitroandin vivoanti-cancer activity ofN-((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.
authors.affiliation: Division of Organic Chemistry, CSIR-National Chemical Laboratory, Pune, India 411008.
authors.forename: Yadagiri
authors.initials: Y
authors.lastname: Kommagalla
authors.affiliation: Department of Developmental, Molecular and Chemical Biology, Tufts University, 136 Harrison Avenue, Boston, MA 02111.
authors.forename: Sinziana
authors.initials: S
authors.lastname: Cornea
authors.affiliation: Department of Pharmaceutical Sciences, Bouve College of Health Sciences, Northeastern University, 140 The Fenway, Boston, MA 02115.
authors.forename: Robert
authors.initials: R
authors.lastname: Riehle
authors.affiliation: Department of Pharmaceutical Sciences, Bouve College of Health Sciences, Northeastern University, 140 The Fenway, Boston, MA 02115.
authors.forename: Vladimir
authors.initials: V
authors.lastname: Torchilin
authors.affiliation: Department of Developmental, Molecular and Chemical Biology, Tufts University, 136 Harrison Avenue, Boston, MA 02111.
authors.forename: Alexei
authors.initials: A
authors.lastname: Degterev
authors.affiliation: Division of Organic Chemistry, CSIR-National Chemical Laboratory, Pune, India 411008.
authors.forename: Chepuri V
authors.initials: CV
authors.lastname: Ramana