Biological evaluation of an antibiotic DC-81-indole conjugate agent in human melanoma cell lines.
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.
Hu
Wan-Ping
WP
School of Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
Yu
Hsin-Su
HS
Chen
Yen-Chi
YC
Wang
Jeh-Jeng
JJ
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
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