Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors

作者：Tang, Qidong^*; Wang, Linxiao; Tu, Yayi; Zhu, Wufu; Luo, Rong; Tu, Qidong; Wang, Ping; Wu, Chunjiang; Gong, Ping; Zheng, Pengwu^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(7): 1680-1684.

DOI：10.1016/j.bmcl.2016.02.059

• Synthesis
• Pyrrolo[2,3-b]pyridine derivatives
• 1,2,3-Triazole
• c-Met
• Antiproliferative activity

A series of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety were designed, synthesized, and evaluated for their c-Met kinase inhibitory activities and antiproliferative activities against 4 cancer cell lines (HT-29, A549, MCF-7, and PC-3) in vitro. Most compounds showed moderate to excellent potency, with the most promising analog 34 showing a c-Met IC50 value of 1.68 nM. Structure-activity relationship studies indicated that electron-withdrawing groups (X = CF3, R-1 = F, R-2 = 4-F) were required to decrease the higher electron density on the 5-atom linker to a proper degree to improve the inhibitory activity.

• 出版日期2016-4-1
• 单位江西科技师范大学; 沈阳药科大学