Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists
Autor: | Hiroshi Koutoku, Masafumi Kudoh, Isao Kinoyama, Toru Yoden, Takashi Furutani, Minoru Okada, Nobuaki Taniguchi |
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Rok vydání: | 2004 |
Předmět: |
Reporter gene
Bicalutamide Antiandrogens Stereochemistry Drug Evaluation Preclinical General Chemistry General Medicine CHO Cells Piperazines Chemical library Androgen receptor chemistry.chemical_compound chemistry Receptors Androgen Cricetinae Drug Discovery medicine Androgen Receptor Antagonists Moiety Animals Humans Lead compound IC50 medicine.drug |
Zdroj: | Chemicalpharmaceutical bulletin. 52(11) |
ISSN: | 0009-2363 |
Popis: | The search for novel antiandrogens by high-throughput screening (HTS) of the Yamanouchi chemical library led to the discovery of the lead compound (5), which possesses an arylmorpholine moiety. Through the optimization of the lead compound (5), we have found a series of novel arylpiperazine derivatives. Among them, 4-[4-cyano-(3-trifluoromethyl)phenyl]-N-(4-fluorophenyl)piperazine-1-carboxamide (22; YM-92088) exhibited a potent AR antagonistic activity with an IC(50) value of 0.47 microM in the reporter assay, which is more potent than bicalutamide (4) which has an IC(50) value of 0.89 microM. |
Databáze: | OpenAIRE |
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