The interaction with tubulin of a series of stilbenes based on combretastatin A-4.

A series of stilbenes, based on combretastatin A-4, were synthesised. A structure-activity study was carried out to characterise the interaction of these agents with tubulin. The substitution of small alkyl substituents for the 4'-methoxy group of combretastatin A-4 and the loss of the 3'-...

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Autores principales: Woods, J. A., Hadfield, J. A., Pettit, G. R., Fox, B. W., McGown, A. T.
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 1995
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2033763/
https://www.ncbi.nlm.nih.gov/pubmed/7710932
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author Woods, J. A.
Hadfield, J. A.
Pettit, G. R.
Fox, B. W.
McGown, A. T.
author_facet Woods, J. A.
Hadfield, J. A.
Pettit, G. R.
Fox, B. W.
McGown, A. T.
author_sort Woods, J. A.
collection PubMed
description A series of stilbenes, based on combretastatin A-4, were synthesised. A structure-activity study was carried out to characterise the interaction of these agents with tubulin. The substitution of small alkyl substituents for the 4'-methoxy group of combretastatin A-4 and the loss of the 3'-hydroxyl group does not have a major effect on the interaction with tubulin. trans-Stilbenes were shown to bind tubulin, but do not inhibit microtubule assembly. This work, together with previous studies, has been used to propose an idealised structure for a tubulin-binding agent of this type. IMAGES:
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spelling pubmed-20337632009-09-10 The interaction with tubulin of a series of stilbenes based on combretastatin A-4. Woods, J. A. Hadfield, J. A. Pettit, G. R. Fox, B. W. McGown, A. T. Br J Cancer Research Article A series of stilbenes, based on combretastatin A-4, were synthesised. A structure-activity study was carried out to characterise the interaction of these agents with tubulin. The substitution of small alkyl substituents for the 4'-methoxy group of combretastatin A-4 and the loss of the 3'-hydroxyl group does not have a major effect on the interaction with tubulin. trans-Stilbenes were shown to bind tubulin, but do not inhibit microtubule assembly. This work, together with previous studies, has been used to propose an idealised structure for a tubulin-binding agent of this type. IMAGES: Nature Publishing Group 1995-04 /pmc/articles/PMC2033763/ /pubmed/7710932 Text en https://creativecommons.org/licenses/by/4.0/This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/.
spellingShingle Research Article
Woods, J. A.
Hadfield, J. A.
Pettit, G. R.
Fox, B. W.
McGown, A. T.
The interaction with tubulin of a series of stilbenes based on combretastatin A-4.
title The interaction with tubulin of a series of stilbenes based on combretastatin A-4.
title_full The interaction with tubulin of a series of stilbenes based on combretastatin A-4.
title_fullStr The interaction with tubulin of a series of stilbenes based on combretastatin A-4.
title_full_unstemmed The interaction with tubulin of a series of stilbenes based on combretastatin A-4.
title_short The interaction with tubulin of a series of stilbenes based on combretastatin A-4.
title_sort interaction with tubulin of a series of stilbenes based on combretastatin a-4.
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2033763/
https://www.ncbi.nlm.nih.gov/pubmed/7710932
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