Abstract
Anti-apoptotic Bcl-2 protects cells from apoptosis by binding to pro-apoptotic members of the Bcl-2 family thereby playing a role in tumour survival in response to chemo- or radiation therapy. We describe a series of phenyl pyrazoles that have high affinity for Bcl-2 and rationalise the observed SAR by means of an X-ray crystal structure.
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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Crystallography, X-Ray
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Molecular Structure
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Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors*
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Pyrazoles / chemical synthesis*
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Pyrazoles / pharmacology
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Structure-Activity Relationship
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Tetrahydroisoquinolines / chemistry*
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Tetrahydroisoquinolines / pharmacology
Substances
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Antineoplastic Agents
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Proto-Oncogene Proteins c-bcl-2
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Pyrazoles
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Tetrahydroisoquinolines