Discovery of indole inhibitors of chemokine receptor 9 (CCR9)
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- 作者：Bhaumik A. Pandya ; pandya.bhaumik@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Christian Baber ; Audrey Chan ; Brian Chamberlain ; Haoqun Chandonnet ; Jennifer Goss ; Timothy Hopper ; Blaise Lippa ; Katherine Poutsiaka ; Jan Romero ; Sabrina Stucka ; Mustafa Varoglu ; Jing Zhang ; Xin Zhang
- 关键词：CCR9 ; chemokine receptor 9 ; CCL25 ; chemokine ligand 25
- 刊名：Bioorganic & Medicinal Chemistry Letters
- 出版年：2016
- 出版时间：15 July 2016
- 年：2016
- 卷：26
- 期：14
- 页码：3322-3325
- 全文大小：1196 K
文摘
Irritable bowel diseases (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC) are serious chronic diseases affecting millions of patients worldwide. Studies of human chemokine biology has suggested C–C chemokine receptor 9 (CCR9) may be a key mediator of pro-inflammatory signaling. Discovery of agents that inhibit CCR9 may lead to new therapies for CD and UC patients. Herein we describe the evolution of a high content screening hit (1) into potent inhibitors of CCR9, such as azaindole 12.