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Design and synthesis of a DNA-crosslinking azinomycin analogue

By Klaus Pors, M.A. Casely-Hayford, J.A. Hartley, Laurence H. Patterson and M. Searcey

Abstract

NoThe azinomycins are potent antitumour antibiotics that are able to crosslink DNA, but are relatively unstable and unlikely to progress as therapeutic candidates. A prototype analogue 4 with more clinical potential has been designed and synthesised and incorporates the epoxide function of the azinomycins and a nitrogen mustard. Two further analogues 5 and 6 that can alkylate DNA but cannot crosslink the duplex have also been synthesised. Compound 4 crosslinks DNA efficiently at nM concentrations. Compounds 4¿6 were submitted to the NCI 60 cell line screen and have similar antitumour activity, although 4 is slightly less active than the non-crosslinking compounds. These observations will be important in the design of further azinomycin analogues with antitumour activity

Topics: DNA-crosslinking, Azinomycin Analogue, Cancer Therapeutics
Year: 2005
DOI identifier: 10.1039/b508908e
OAI identifier: oai:bradscholars.brad.ac.uk:10454/4115
Provided by: Bradford Scholars
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