Abstract
A series of ageladine A analogs that include 2-aminoimidazo[4,5-c]azepines (seven-membered rings) and 2-amino-3H-imidazo[4,5-c]pyridine (six-membered rings) derivatives were synthesized and evaluated for their anticancer effects against several human cancer cell lines and MMP-2 inhibition in vitro. Only compounds possessing the aromatic azepine (seven-membered ring) core showed anticancer activity with IC(50) values in the low micromolar range.
Copyright 2009 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Humans
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Imidazoles / chemistry
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Matrix Metalloproteinase 2 / metabolism
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Matrix Metalloproteinase Inhibitors
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Oxidation-Reduction
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Pyrroles / chemical synthesis
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Pyrroles / chemistry*
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Pyrroles / pharmacology
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Structure-Activity Relationship
Substances
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Ageladine A
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Antineoplastic Agents
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Imidazoles
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Matrix Metalloproteinase Inhibitors
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Pyrroles
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2-aminoimidazole
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Matrix Metalloproteinase 2
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oroidin