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Design and synthesis of a DNA-crosslinking azinomycin analogue

Pors, Klaus
Casely-Hayford, M.A.
Hartley, J.A.
Patterson, Laurence H.
Searcey, M.
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2005
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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. 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.
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Pors, K., Casely-Hayford, M., Hartley, J.A. and Patterson, L.H. (2005). Design and synthesis of a DNA-crosslinking azinomycin analogue. Organic & Biomolecular Chemistry. Vol. 3, No. 19, pp. 3585-3589.
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