The synthesis and evaluation of benzannelated-azatoxins: The benzazatoxins

The synthesis and evaluation of azatoxin congeners possessing annealed aromatic frameworks are described. The compounds were evaluated for their abilities to affect topoisomerase II inhibition through the stabilization of “cleavable complex” and for the inhibition of tubulin polymerization using pur...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-05, Vol.8 (9), p.1065-1070
Main Authors: Miller, Thomas A., Vachaspati, Prakash R., Labroli, Marc A., Thompson, Charles D., Bulman, Amanda L., Macdonald, Timothy L.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Biological and medical sciences
Brain - metabolism
Cattle
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
General aspects
Indicators and Reagents
Indoles - chemical synthesis
Indoles - chemistry
Indoles - pharmacology
Kinetics
Medical sciences
Molecular Conformation
Molecular Structure
Pharmacology. Drug treatments
Quinoxalines - chemical synthesis
Quinoxalines - chemistry
Quinoxalines - pharmacology
Structure-Activity Relationship
Topoisomerase II Inhibitors
Tubulin - drug effects
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Summary:The synthesis and evaluation of azatoxin congeners possessing annealed aromatic frameworks are described. The compounds were evaluated for their abilities to affect topoisomerase II inhibition through the stabilization of “cleavable complex” and for the inhibition of tubulin polymerization using purified bovine brain tubulin. The synthesis and evaluation of azatoxin congeners possessing annealed aromatic frameworks are described. The compounds were evaluated for their abilities to affect topoisomerase II inhibition through the stabilization of “cleavable complex” and for the inhibition of tubulin polymerization using purified bovine brain tubulin.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00176-0