Abstract
Here we report that 6-hydroximino-4-aza-A-homo-cholest-3-one and 6-hydroxyl-4-aza-A-homo-cholest-3-one, new steroidal lactams were synthesized recently, displayed antiproliferative activity against some cancer cells through inducing cancer cell apoptosis by activation of the intrinsic pathway. The apoptotic function of the compounds was demonstrated by release of cytochrome C, activation of caspase 3 and annexin V labeling. Furthermore, the compound was able to inhibit tumor growth in an athymic mouse model.
Copyright © 2012 Elsevier Inc. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Annexin A5 / metabolism
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use*
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Apoptosis / drug effects*
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Blotting, Western
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Caspase 3 / metabolism
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Cell Proliferation / drug effects
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Cytochromes c / metabolism
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HT29 Cells
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Humans
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Lactams / chemistry
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Lactams / pharmacology*
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Lactams / therapeutic use*
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Mice
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Mice, Nude
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Steroids / chemistry
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Steroids / pharmacology*
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Steroids / therapeutic use*
Substances
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Annexin A5
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Antineoplastic Agents
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Lactams
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Steroids
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Cytochromes c
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Caspase 3