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Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?

Gaukroger, K, Hadfield, JA, Lawrence, NJ, Nolan, S and McGown, AT 2003, 'Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?' , Organic and Biomolecular Chemistry, 1 (17) , pp. 3033-3037.

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Abstract

A series of combretastatins possessing both a trimethoxy unit and other substituents on ring A has been synthesised and tested for cytotoxicity and their ability to interact with the protein tubulin. All previous studies have indicated that the trimethoxy unit is essential for interaction with tubulin. The studies herein show that molecules possessing functionalities other than trimethoxy can also interact with tubulin. Importantly a trimethyl substituted agent 52a has shown reduced cytotoxicity, but increased potency in its ability to inhibit the assembly of tubulin.

Item Type: Article
Themes: Subjects / Themes > Q Science > Q Science (General)
Subjects / Themes > Q Science > QD Chemistry
Subjects outside of the University Themes
Schools: Colleges and Schools > College of Science & Technology
Colleges and Schools > College of Science & Technology > School of Environment and Life Sciences
Colleges and Schools > College of Science & Technology > School of Environment and Life Sciences > Biomedical Research Centre
Journal or Publication Title: Organic and Biomolecular Chemistry
Publisher: Royal Society of Chemistry
Refereed: Yes
ISSN: 14770520
Depositing User: H Kenna
Date Deposited: 07 Aug 2007 14:54
Last Modified: 20 Aug 2013 16:45
URI: http://usir.salford.ac.uk/id/eprint/150

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