A new anti-tubulin agent containing the benzo[ b]thiophene ring system

A new type of inhibitor of tubulin polymerization was discovered based on the 3-aroyl-2-arylbenzo[ b]thiophene molecular skeleton. The lead compound in this series, 2-(4′-methoxyphenyl)-3-(3′,4′,5′-trimethoxybenzoyl)-6-methoxybenzo[ b]thiophene 1, inhibited tubulin polymerization, caused an increase...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-04, Vol.9 (8), p.1081-1086
Main Authors: Pinney, Kevin G., Bounds, A.Dawn, Dingeman, Koren M., Mocharla, Vani P., Pettit, George R., Bai, Ruoli, Hamel, Ernest
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
Dose-Response Relationship, Drug
General aspects
Humans
Hydrolysis - drug effects
Medical sciences
Pharmacology. Drug treatments
Thiophenes - chemistry
Time Factors
Tubulin - chemical synthesis
Tubulin - pharmacology
Tubulin Modulators
Tumor Cells, Cultured
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Summary:A new type of inhibitor of tubulin polymerization was discovered based on the 3-aroyl-2-arylbenzo[ b]thiophene molecular skeleton. The lead compound in this series, 2-(4′-methoxyphenyl)-3-(3′,4′,5′-trimethoxybenzoyl)-6-methoxybenzo[ b]thiophene 1, inhibited tubulin polymerization, caused an increase in the mitotic index of CA46 Burkitt lymphoma cells, and inhibited the growth of several human cancer cell lines. A new type of inhibitor of tubulin polymerization was discovered based on the 3-aroyl-2-arylbenzol[ b]thiophene molecular skeleton. The lead compound in this series, benzo[ b]thiophene 1, inhibited tubulin polymerization, caused an increase in the mitotic index of CA46 Burkitt lymphoma cells, and inhibited the growth of several human cancer cell lines.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00143-2