Abstract
A series of phenylacylsulfonamides has been prepared as antagonists of Bcl-2/Bcl-xL. In addition to potent binding affinities for both Bcl-2 and Bcl-xL, these compounds were shown to induce classical markers of apoptosis in isolated mitochondria. Overall weak cellular potency was improved by the incorporation of polar functionality resulting in compounds with moderate antiproliferative activity.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Apoptosis / drug effects
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Cell Line, Tumor
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Crystallography, X-Ray
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Cytochromes c / metabolism
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Humans
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Hydrophobic and Hydrophilic Interactions
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Mitochondria / drug effects*
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Mitochondria / metabolism
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Models, Molecular
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Sulfonamides / chemical synthesis*
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Sulfonamides / pharmacology
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bcl-2-Associated X Protein / antagonists & inhibitors*
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bcl-2-Associated X Protein / chemistry
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bcl-X Protein / antagonists & inhibitors*
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bcl-X Protein / chemistry
Substances
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Antineoplastic Agents
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Sulfonamides
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bcl-2-Associated X Protein
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bcl-X Protein
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Cytochromes c