Issue 17, 2003
From the journal:

Organic & Biomolecular Chemistry

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

Keira Gaukroger,a   John A Hadfield,*ab   Nicholas J Lawrence,cd   Steven Nolana  and  Alan T McGownab  

* Corresponding authors

a Drug Development Section, Paterson Institute for Cancer Research, Christie Hospital NHS Trust, Wilmslow Road, Manchester

b Centre for Molecular Drug Design, Cockcroft Building, University of Salford, Manchester

c Department of Chemistry, UMIST, PO Box 88, Manchester

d Department of Chemistry, Cardiff University, PO Box 912, Cardiff

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.

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

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Article information

DOI
https://doi.org/10.1039/B306878A
Article type
Paper
Submitted
19 Jun 2003
Accepted
09 Jul 2003
First published
24 Jul 2003

Org. Biomol. Chem., 2003,1, 3033-3037

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

K. Gaukroger, J. A. Hadfield, N. J. Lawrence, S. Nolan and A. T. McGown, Org. Biomol. Chem., 2003, 1, 3033 DOI: 10.1039/B306878A

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