Truncated azinomycin analogues intercalate into DNA.

Description

No / The design and synthesis of a potentially more therapeutically-viable azinomycin analogue 4 based upon 3 has been completed. It involved coupling of a piperidine mustard to the acid chloride of the azinomycin chromophore. Both the designed azinomycin analogue 4 and the natural product 3 bind to DNA and cause unwinding, supporting an intercalative mode of binding.

Graphical abstract
A designed analogue of the left half of azinomycin has been synthesized and unwinds supercoiled DNA.

Links & Downloads

1. Casely-Hayward, M., Pors, K., Patterson, L.H. and Gerner, C. et al. (2005). Truncated azinomycin analogues intercalate into DNA. Bioorganic Medicinal Chemistry Letters. Vol. 15, No. 3, pp. 653-656.
2. http://hdl.handle.net/10454/3908
3. https://doi.org/10.1016/j.bmcl.2004.11.037

Tags

Azinomycin

Intercalation;

DNA unwinding

Synthesis

Analogues

Additional Fields

Identifer	oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/3908
Date	January 2005
Creators	Casely-Hayford, M.A., Pors, Klaus, Patterson, Laurence H., Gerner, C., Neidle, S., Searcey, M.
Source Sets	Bradford Scholars
Language	English
Detected Language	English
Type	Article, No full-text available in the repository