title: Biological evaluation of an antibiotic DC-81-indole conjugate agent in human melanoma cell lines.
abstract: Pyrrolo[2, 1-c][1, 4]benzodiazepines (PBDs) are potent inhibitors of nucleic acid synthesis because of their ability to recognize and bind to specific sequences of DNA and form a labile covalent adduct. DC-81, an antitumor antibiotic produced by Streptomyces species, is a PBD. We combined DC-81 and an indole carboxylate moiety to synthesize a hybrid designed to have much higher sequence selectivity in DNA interactivity. In this paper, the cytotoxic potency of the hybrid in human melanoma cell lines was studied. XTT assay demonstrated that the DC-81-indole conjugate possessed cytotoxicity against human melanoma cell lines.
authors.affiliation: School of Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
authors.forename: Wan-Ping
authors.initials: WP
authors.lastname: Hu
authors.forename: Hsin-Su
authors.initials: HS
authors.lastname: Yu
authors.forename: Yen-Chi
authors.initials: YC
authors.lastname: Chen
authors.forename: Jeh-Jeng
authors.initials: JJ
authors.lastname: Wang
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D001569:Benzodiazepines / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism; D006801:Humans; D008545:Melanoma / Q000188:drug therapy* / Q000473:pathology; D009943:Organophosphorus Compounds; D011758:Pyrroles / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: C474072:(11aS)-8-hydroxy-7-methoxy-1,2,3,11a-tetrahydro-5H-pyrrolo(2,1-c)(1,4)benzodiazepin-5-one; D000903:Antibiotics, Antineoplastic; D009943:Organophosphorus Compounds; D011758:Pyrroles; C438462:pyrrolo(2,1-c)(1,4)benzodiazepine; D001569:Benzodiazepines; D004247:DNA