Abstract
In this study, we synthesized the BF-3 binding small molecules, a series of pyridazinone-based compounds, as a novel class of non-LBP antiandrogens for treating prostate cancer by inhibiting androgen receptor. The new class compound was discovered to inhibitor the viability of AR-dependent human prostate LNCap cells and AR activity combining with the computational method. It showed a good physicochemical and PK property.
Copyright © 2013 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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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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Dose-Response Relationship, Drug
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Drug Discovery*
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Drug Screening Assays, Antitumor
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Humans
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Male
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Models, Molecular
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Molecular Structure
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Prostatic Neoplasms / drug therapy*
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Prostatic Neoplasms / pathology
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Pyridazines / administration & dosage
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Pyridazines / chemistry
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Pyridazines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Receptors, Androgen / metabolism*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Pyridazines
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Receptors, Androgen