Abstract
Anti-apoptotic Bcl-2 family proteins such as Bcl-2 and Bcl-X(L) have been recently validated as targets for the discovery of novel anti-cancer agents. We previously reported that racemic (+/-) Apogossypol, a semi-synthetic compound derived from the natural product Gossypol, binds and inhibits Bcl-2 and Bcl-X(L)in vitro and in cell. Given that (+) and (-) Gossypol display different proapoptotic activities, here we report on the synthesis of (+) and (-) Apogossypol and the evaluation of their in vitro and cellular activity.
Publication types
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Evaluation Study
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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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Cell Survival / drug effects
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Fluorescence Polarization
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Gossypol / analogs & derivatives*
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Gossypol / chemical synthesis
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Gossypol / pharmacology
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Humans
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Molecular Structure
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Stereoisomerism
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bcl-X Protein / antagonists & inhibitors*
Substances
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Antineoplastic Agents
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apogossypol
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bcl-X Protein
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Gossypol