Abstract
Synthesis and broad-spectrum anticancer activity of a novel heterocyclic compound 1 containing the title imidazo[4,5-e][1,3]diazepine ring system have been reported. The compound shows potent in vitro antitumor activity with low micromolar IC(50)'s against prostate, lung, breast, and ovarian cancer cell lines tested. The long alkyl chain attached to the six-position of the heterocyclic ring of 1 appears to be necessary for the observed biological activity.
Copyright 2010 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / therapeutic use
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Azepines / chemistry*
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Breast Neoplasms / drug therapy
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Female
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / chemistry*
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Heterocyclic Compounds / therapeutic use
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Humans
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Lung Neoplasms / drug therapy
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Male
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Neoplasms / drug therapy*
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Ovarian Neoplasms / drug therapy
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Prostatic Neoplasms / drug therapy
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Azepines
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Heterocyclic Compounds