Design, synthesis, and evaluation of potent Wnt signaling inhibitors featuring a fused 3-ring system
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- 作者：Zhixiang Xua ; 1 ; Jiajun Lia ; 1 ; Yiyuan Wub ; Zhijian Sunb ; Lusong Luob ; lusong.luo@beigene.com" class="auth_mail" title="E-mail the corresponding author ; Zhilin Huc ; Sudan Hec ; Jiyue Zhenga ; jyzheng@suda.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Hongjian Zhanga ; Xiaohu Zhanga ; xiaohuzhang@suda.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Wnt signaling pathway ; Porcupine ; Antagonist ; Scaffold hybridization ; Cancer therapy
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：154-165
- 全文大小：1018 K
文摘
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A novel series of Wnt antagonists were developed by a scaffold hybridization strategy.
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Many compounds exhibited Wnt inhibition at low nM range.
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Compound class="boldFont">59 showed excellent chemical, plasma, and liver microsomal stability.
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Compound class="boldFont">59 demonstrated good PK profiles with 30% oral bioavailability in rat.