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Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists.
Wu, Tian-Ming; Wang, Dao-Cai; Xiang, Pu; Zhang, Jian-Nan; Sang, Ya-Xiong; Lin, Hong-Jun; Chen, Jie; Xie, Gang; Song, Hang; Zhao, Ying-Lan; Xie, Yong-Mei.
Afiliación
  • Wu TM; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Wang DC; Department of Pharmaceutical and Biological Engineering, College of Chemical Engineering, Sichuan University, Chengdu 610065, China.
  • Xiang P; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Zhang JN; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Sang YX; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Lin HJ; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Chen J; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Xie G; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
  • Song H; Department of Pharmaceutical and Biological Engineering, College of Chemical Engineering, Sichuan University, Chengdu 610065, China.
  • Zhao YL; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China. Electronic address: zhaoyinglan@scu.edu.cn.
  • Xie YM; State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China. Electronic address: xieym@scu.edu.cn.
Bioorg Med Chem Lett ; 24(5): 1426-31, 2014 Mar 01.
Article en En | MEDLINE | ID: mdl-24491459
ABSTRACT
A series of novel benzamide derivatives were prepared and evaluated using cell-based measurements. Among these compounds, 10f significantly inhibited Hedgehog signaling and showed equivalent or more potency than GDC-0449 in different tests. Furthermore, compound 10f potently inhibited the proliferation of Daoy, a medulloblastoma cell line that is reported to be resistant to GDC-0449, which indicated a promising prospect in the treatment of Hedgehog signaling pathway related cancer in clinical trial.
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Sulfonas / Benzamidas / Transducción de Señal / Receptores Acoplados a Proteínas G Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article
Texto completo
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Texto completo: 1 Base de datos: MEDLINE Asunto principal: Sulfonas / Benzamidas / Transducción de Señal / Receptores Acoplados a Proteínas G Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2014 Tipo del documento: Article