Design and synthesis of a DNA-crosslinking azinomycin analogue

MA Casely-Hayford, K Pors, CH James…

Index: Casely-Hayford, Maxwell A.; Pors, Klaus; James, Colin H.; Patterson, Laurence H.; Hartley, John A.; Searcey, Mark Organic and Biomolecular Chemistry, 2005 , vol. 3, # 19 p. 3585 - 3589

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Citation Number: 21

Abstract

The 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. ...