K Gaukroger
Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?
Gaukroger, K; Hadfield, JA; Lawrence, NJ; Nolan, S; McGown, AT
Authors
JA Hadfield
NJ Lawrence
S Nolan
AT McGown
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.
Citation
Gaukroger, K., Hadfield, J., Lawrence, N., Nolan, S., & McGown, A. (2003). Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?. Organic and Biomolecular Chemistry, 1(17), 3033-3037. https://doi.org/10.1039/b306878a
Journal Article Type | Article |
---|---|
Publication Date | Jul 1, 2003 |
Deposit Date | Aug 7, 2007 |
Journal | Organic and Biomolecular Chemistry |
Print ISSN | 1477-0520 |
Publisher | Royal Society of Chemistry |
Peer Reviewed | Peer Reviewed |
Volume | 1 |
Issue | 17 |
Pages | 3033-3037 |
DOI | https://doi.org/10.1039/b306878a |
Publisher URL | http://dx.doi.org/10.1039/b306878a |
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