Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?
Gaukroger, Keira Hadfield, John A Lawrence, Nicholas J Nolan, Steven McGown, Alan T
Gaukroger, Keira
Hadfield, John A
Lawrence, Nicholas J
Nolan, Steven
McGown, Alan T
Citations
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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.
Description
Date
2003-09-07
Publisher
Collections
Keywords
Antitumour Drug Screening Assays
Type
Article
Citation
Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit? 2003, 1 (17):3033-7 Org. Biomol. Chem.