Design, synthesis, and biological evaluation of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives as androgen receptor antagonists

Journal Article · Fri Mar 15 00:00:00 EDT 2019 · Medicinal Chemistry Research (Print)

DOI:https://doi.org/10.1007/S00044-019-02291-Y· OSTI ID:22936205

Dong, Junze; Zhang, Jingya; Li, Zilu ^[1]; Asnake, Solomon ^[2]; Zhang, Daoguang ^[1]; Olsson, Per-Erik ^[2]; Zhao, Guisen ^[1]

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1. Shandong University, Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences (China)
2. Örebro University, Biology, The Life Science Center, School of Science and Technology (Sweden)

Androgen receptor (AR) signaling is often activated in prostate cancer (PCa) cells, and blockage of this signaling by AR antagonists is an important strategy in PCa therapy. In this study, we designed and synthesized a series of 2-(5-methyl-1H-pyrazol-1-yl) acetamide derivatives, and evaluated their biological activities. AR luciferase reporter assay revealed compound 6f (59.7%) as a potent AR antagonist. Some compounds in this series showed higher anti-proliferative activity against LNCaP cells than Bicalutamide (IC{sub 50} = 35.0 μM), especially 6g with IC{sub 50} value of 13.6 μM.

• OSTI ID: 22936205
• Journal Information: Medicinal Chemistry Research (Print), Journal Name: Medicinal Chemistry Research (Print) Journal Issue: 3 Vol. 28; ISSN 1054-2523
• Country of Publication: United States
• Language: English

Related Subjects

60 APPLIED LIFE SCIENCES
ACETAMIDE
ANDROGENS
LUCIFERASE
NEOPLASMS
PROSTATE
PYRAZOLES
RECEPTORS
SYNTHESIS
THERAPY