Synthesis of novel C2-aryl pyrrolobenzodiazepines (PBDs) as potential antitumour agents.
Three novel C2-aryl substituted pyrrolobenzodiazepines (PBDs) have been synthesised and evaluated in a number of cell lines revealing selective cytotoxicity at the sub-nanomolar level towards melanoma and ovarian cancer cell lines.
CRUK Gene Targeted Drug Design Research Group, School of Pharmacy, University of London, 29/39 Brunswick Square, London, UK WC1N 1AX.
Nectaroula
N
Cooper
David R
DR
Hagan
Arnaud
A
Tiberghien
Temitope
T
Ademefun
Charles S
CS
Matthews
Philip W
PW
Howard
David E
DE
Thurston
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D008297:Male; D008545:Melanoma / Q000188:drug therapy / Q000473:pathology; D010051:Ovarian Neoplasms / Q000188:drug therapy / Q000473:pathology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D011758:Pyrroles; C438462:pyrrolo(2,1-c)(1,4)benzodiazepine; D001569:Benzodiazepines