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

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

  • Bioorg Med Chem Lett. 2016 Apr 1;26(7):1680-4. doi: 10.1016/j.bmcl.2016.02.059.
Qidong Tang 1,  Linxiao Wang 2,  Yayi Tu 2,  Wufu Zhu 2,  Rong Luo 3,  Qidong Tu 2,  Ping Wang 2,  Chunjiang Wu 2,  Ping Gong 4,  Pengwu Zheng 5
Affiliations

Affiliations

  • 1 School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, PR China; Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China. Electronic address: tangqidongcn@126.com.
  • 2 School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, PR China.
  • 3 Jiangxi Province Institute of Materia Medica, Nanchang 330000, PR China.
  • 4 Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, PR China.
  • 5 School of Pharmacy, Jiangxi Science and Technology Normal University, Nanchang 330013, PR China. Electronic address: zhengpw@126.com.
PMID: 26923692 DOI: 10.1016/j.bmcl.2016.02.059
Abstract

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 1.68nM. 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.

Keywords

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

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