Caulerpenyne–colchicine hybrid: Synthesis and biological evaluation

The synthesis of an analog of caulerpenyne having a trimethoxyaryl moiety was achieved in 11% overall yield over 11 steps. Its biological activity has been evaluated as inhibitor of in vitro tubulin polymerization or angiogenesis.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2006-08, Vol.14 (16), p.5540-5548
Main Authors: Bourdron, Julien, Commeiras, Laurent, Barbier, Pascale, Bourgarel-Rey, Véronique, Pasquier, Eddy, Vanthuyne, Nicolas, Hubaud, Jean-Claude, Peyrot, Vincent, Parrain, Jean-Luc
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Biological evaluation
Caulerpenyne
Cell cytotoxicity
Cell Line, Tumor
Chemical Sciences
Colchicine
Colchicine - analogs & derivatives
Colchicine - chemical synthesis
Colchicine - pharmacology
Drug Screening Assays, Antitumor
General aspects
Humans
In vitro angiogenesis
Medical sciences
Medicinal Chemistry
Neovascularization, Physiologic - drug effects
Neovascularization, Physiologic - physiology
Pharmacology. Drug treatments
Polymers - chemistry
Sesquiterpenes - chemical synthesis
Sesquiterpenes - pharmacology
Structure-Activity Relationship
Tubulin - drug effects
Tubulin - metabolism
Tubulin polymerization
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Description
Summary:The synthesis of an analog of caulerpenyne having a trimethoxyaryl moiety was achieved in 11% overall yield over 11 steps. Its biological activity has been evaluated as inhibitor of in vitro tubulin polymerization or angiogenesis.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.04.024