Azinomycin inspired bisepoxides: influence of linker structure on in vitro cytotoxicity and DNA interstrand cross-linking.
A series of bisepoxides based on the epoxide domain of the naturally occurring azinomycins have been synthesised. The incorporation of an aminomethyl group into the linker between the two alkylating epoxide units is shown to significantly enhance in vitro cytotoxicity against human tumour cell lines and DNA interstand cross-linking efficiency.
LePla
Rachel C
RC
Department of Chemistry, University of Warwick, Coventry, UK.
Landreau
Cyrille A S
CA
Shipman
Michael
M
Hartley
John A
JA
Jones
George D D
GD
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D053961:Azabicyclo Compounds; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D004151:Dipeptides; D004591:Electrophoresis, Polyacrylamide Gel; D004852:Epoxy Compounds / Q000737:chemistry*; D006020:Glycopeptides / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins; D009281:Naphthalenes / Q000737:chemistry / Q000494:pharmacology; D010455:Peptides
D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D053961:Azabicyclo Compounds; D004151:Dipeptides; D004852:Epoxy Compounds; D006020:Glycopeptides; D036341:Intercellular Signaling Peptides and Proteins; D009281:Naphthalenes; D010455:Peptides; C051055:azinomycin B; C051054:azinomycin A; D004247:DNA