The synthesis of amino-acid functionalized β-Carbolines as topoisomerase II inhibitors

The synthesis of amino-acid functionalized β-Carbolines as topoisomerase II inhibitors

The synthesis and biological activity of amino acid functionalized β-carboline derivatives, which are structurally related to azatoxin and the tryprostatins, are reported. These compounds were assayed for their growth inhibition properties in H520 and PC3 cell lines and were examined for their abili...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-05, Vol.11 (10), p.1251-1255
Hauptverfasser: Deveau, Amy Morin, Labroli, Marc A, Dieckhaus, Christine M, Barthen, Mary T, Smith, Kirsten S, Macdonald, Timothy L
Format: Artikel
Sprache:eng
Schlagworte:
Amino Acids - chemistry
Amino Acids - pharmacology
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Carbolines - chemical synthesis
Carbolines - pharmacology
Cell Division - drug effects
Dose-Response Relationship, Drug
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - pharmacology
General aspects
Humans
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
Topoisomerase II Inhibitors
Tumor Cells, Cultured - drug effects
Tumor Cells, Cultured - enzymology
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Zusammenfassung:The synthesis and biological activity of amino acid functionalized β-carboline derivatives, which are structurally related to azatoxin and the tryprostatins, are reported. These compounds were assayed for their growth inhibition properties in H520 and PC3 cell lines and were examined for their abilities to inhibit topoisomerase II-mediated DNA relaxation. The synthesis and biological activity of amino acid functionalized β-carboline derivatives, which are structurally related to azatoxin and the tryprostatins, are reported. These compounds were assayed for their growth inhibition properties in H520 and PC3 cell lines and were examined for their abilities to inhibit topoisomerase II-mediated DNA relaxation.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00136-6