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

2.50
Hdl Handle:
http://hdl.handle.net/10541/82347
Title:
Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?
Authors:
Gaukroger, Keira; Hadfield, John A; Lawrence, Nicholas J; Nolan, Steven; McGown, Alan T
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.
Affiliation:
Drug Development Section, Paterson Institute for Cancer Research, Christie Hospital NHS Trust, Wilmslow Road, Manchester, M20 4BX.
Citation:
Structural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit? 2003, 1 (17):3033-7 Org. Biomol. Chem.
Journal:
Organic & Biomolecular Chemistry
Issue Date:
7-Sep-2003
URI:
http://hdl.handle.net/10541/82347
PubMed ID:
14518125
Type:
Article
Language:
en
ISSN:
1477-0520
Appears in Collections:
All Paterson Institute for Cancer Research

Full metadata record

DC FieldValue Language
dc.contributor.authorGaukroger, Keira-
dc.contributor.authorHadfield, John A-
dc.contributor.authorLawrence, Nicholas J-
dc.contributor.authorNolan, Steven-
dc.contributor.authorMcGown, Alan T-
dc.date.accessioned2009-09-23T14:08:05Z-
dc.date.available2009-09-23T14:08:05Z-
dc.date.issued2003-09-07-
dc.identifier.citationStructural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit? 2003, 1 (17):3033-7 Org. Biomol. Chem.en
dc.identifier.issn1477-0520-
dc.identifier.pmid14518125-
dc.identifier.urihttp://hdl.handle.net/10541/82347-
dc.description.abstractA 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.en
dc.language.isoenen
dc.subjectAntitumour Drug Screening Assaysen
dc.subject.meshAnimals-
dc.subject.meshAntineoplastic Agents-
dc.subject.meshBibenzyls-
dc.subject.meshCell Line-
dc.subject.meshCercopithecus aethiops-
dc.subject.meshDrug Screening Assays, Antitumor-
dc.subject.meshHumans-
dc.subject.meshImmunohistochemistry-
dc.subject.meshInhibitory Concentration 50-
dc.subject.meshK562 Cells-
dc.subject.meshMolecular Structure-
dc.subject.meshStilbenes-
dc.subject.meshStructure-Activity Relationship-
dc.subject.meshTubulin-
dc.subject.meshVero Cells-
dc.titleStructural requirements for the interaction of combretastatins with tubulin: how important is the trimethoxy unit?en
dc.typeArticleen
dc.contributor.departmentDrug Development Section, Paterson Institute for Cancer Research, Christie Hospital NHS Trust, Wilmslow Road, Manchester, M20 4BX.en
dc.identifier.journalOrganic & Biomolecular Chemistryen

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