Synthesis and evaluation of double bond substituted combretastatins

A series of combretastatins substituted with epoxides, amides and small alkyl groups has been synthesised and evaluated for cytotoxicity and their ability to inhibit the assembly of tubulin. The methyl and ethyl substituted phenols 36, 44 have shown potent antimitotic effects whilst exhibiting reduc...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2005-06, Vol.40 (6), p.529-541
Main Authors: Hadfield, John A., Gaukroger, Keira, Hirst, Nicholas, Weston, Anna P., Lawrence, Nicholas J., McGown, Alan T.
Format: Article
Language:English
Subjects:
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Antimitotic
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Bibenzyls - chemical synthesis
Bibenzyls - chemistry
Bibenzyls - pharmacology
Biological and medical sciences
Cell Cycle - drug effects
Cell Survival - drug effects
Combretastatin
Epoxy Compounds - chemical synthesis
Epoxy Compounds - chemistry
Epoxy Compounds - pharmacology
Formazans - chemistry
General aspects
Humans
Inhibitory Concentration 50
K562 Cells
Magnetic Resonance Spectroscopy
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Spectrophotometry, Ultraviolet
Stilbenes - chemical synthesis
Stilbenes - chemistry
Stilbenes - pharmacology
Tetrazolium Salts - chemistry
Tubulin
Tubulin - metabolism
Tubulin Modulators
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Summary:A series of combretastatins substituted with epoxides, amides and small alkyl groups has been synthesised and evaluated for cytotoxicity and their ability to inhibit the assembly of tubulin. The methyl and ethyl substituted phenols 36, 44 have shown potent antimitotic effects whilst exhibiting reduced cytotoxicity.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2004.12.008