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Casely-Hayford, Maxwell A., Pors, Klaus, James, Colin H., Patterson, Laurence H., Hartley, John A. and Searcey, Mark 
ORCID: https://orcid.org/0000-0003-2273-8949
(2005)
Design and synthesis of a DNA-crosslinking azinomycin analogue.
Organic & Biomolecular Chemistry, 3 (19).
pp. 3585-3589.
ISSN 1477-0520
Abstract
The azinomycins are potent antitumour 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.
| Item Type: | Article |
|---|---|
| Faculty \ School: | Faculty of Science > School of Pharmacy |
| UEA Research Groups: | Faculty of Science > Research Groups > Medicinal Chemistry (former - to 2017) Faculty of Science > Research Groups > Chemical Biology and Medicinal Chemistry (former - to 2021) |
| Depositing User: | Rachel Smith |
| Date Deposited: | 13 Jun 2011 13:35 |
| Last Modified: | 24 Oct 2022 02:16 |
| URI: | https://ueaeprints.uea.ac.uk/id/eprint/32136 |
| DOI: | 10.1039/b508908e |
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