Abstract
A series of small molecule STAT3 inhibitors originally derived from our lead compound STA 21 were synthesized and evaluated. The most potent compound in this series, compound 1, exhibited the same anti-proliferative activities as STA 21 against prostate cancer cell lines that express constitutively active STAT3. Molecular docking showed compound 1 bound to the STAT3beta SH2 domain in a similar manner as STA 21.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anthraquinones / chemical synthesis
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Anthraquinones / chemistry*
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Anthraquinones / pharmacology*
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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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Benz(a)Anthracenes / chemical synthesis
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Benz(a)Anthracenes / chemistry*
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Benz(a)Anthracenes / pharmacology*
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Breast Neoplasms / drug therapy
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Breast Neoplasms / metabolism
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Breast Neoplasms / pathology
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Cell Growth Processes / drug effects
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Cell Line, Tumor
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Drug Design
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Humans
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Hydrogen Bonding
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Inhibitory Concentration 50
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Male
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Models, Molecular
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Prostatic Neoplasms / drug therapy
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Prostatic Neoplasms / metabolism
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Prostatic Neoplasms / pathology
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STAT3 Transcription Factor / antagonists & inhibitors*
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Structure-Activity Relationship
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src Homology Domains
Substances
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Anthraquinones
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Antineoplastic Agents
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Benz(a)Anthracenes
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STAT3 Transcription Factor
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STAT3 protein, human