title: Synthesis of 1,2,3-triazole-linked pyrrolobenzodiazepine conjugates employing 'click' chemistry: DNA-binding affinity and anticancer activity.
abstract: 1,2,3-Triazole based molecules are useful pharmacophores for several DNA-alkylating and cross-linking agents. A series of A/C8, C/C2 and A/C8-C/C2-linked 1,2,3-triazole-PBD conjugates have been synthesized by employing 'click' chemistry. These molecules have exhibited promising DNA-binding affinity and anticancer activity in selected human cancer cell lines.
authors.affiliation: Biotransformation Laboratory, Division of Organic Chemistry, Indian Institute of Chemical Technology, Hyderabad 500 007, India.
authors.forename: Ahmed
authors.initials: A
authors.lastname: Kamal
authors.forename: N
authors.initials: N
authors.lastname: Shankaraiah
authors.forename: V
authors.initials: V
authors.lastname: Devaiah
authors.forename: K
authors.initials: K
authors.lastname: Laxma Reddy
authors.forename: Aarti
authors.initials: A
authors.lastname: Juvekar
authors.forename: Subrata
authors.initials: S
authors.lastname: Sen
authors.forename: Nisha
authors.initials: N
authors.lastname: Kurian
authors.forename: Surekha
authors.initials: S
authors.lastname: Zingde
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D009369:Neoplasms / Q000188:drug therapy / Q000235:genetics; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D011758:Pyrroles; D014230:Triazoles; C438462:pyrrolo(2,1-c)(1,4)benzodiazepine; D001569:Benzodiazepines; D004247:DNA; C427203:calf thymus DNA