2. Academic Validation
  3. Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety as potential antitumor inhibitor

Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety as potential antitumor inhibitor

  • Bioorg Med Chem Lett. 2020 Jan 15;30(2):126848. doi: 10.1016/j.bmcl.2019.126848.
Huimin Liu 1,  Yongli Duan 2,  Hehua Xiong 3,  Jianqing Zhang 3,  Shunmin Huang 3,  Ting Chen 3,  Pengwu Zheng 4,  Qidong Tang 5
Affiliations

Affiliations

  • 1 School of Perfume and Aroma Technology, Shanghai Institute of Technology; Engineering Research Center of Perfume & Aroma and Cosmetics of Ministry of Education, Shanghai 201418, PR China.
  • 2 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China; School of Optoelectronic Science and Engineering, University of Electronic Science and Technology of China (UESTC), Chengdu 610054, PR China.
  • 3 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China.
  • 4 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China. Electronic address: zhengpw@126.com.
  • 5 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China. Electronic address: tangqidongcn@126.com.
PMID: 31836443 DOI: 10.1016/j.bmcl.2019.126848
Abstract

A series of pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety were designed, synthesized and evaluated for the anti-proliferative on three Cancer cell lines (A549, HepG2 and MCF-7) in vitro. Most of the compounds showed moderate to high potency. Some excellent compounds were tested for the inhibitory activity of c-Met kinase. Compound 34 (c-Met IC50 = 17 nM) was investigated the selectivity against Flt-3, c-Kit, VEGFR-2, ALK, PDGFR-β and RON. Structure-activity relationship studies indicated that hydrogen, fluorine atom, and mono-electron-withdrawing groups (mono-EWGs, such as R2 = F) on R, R1 and R2, respectively, were beneficial for the anti-proliferative activities of the target compounds. Besides, we have took further study on the combined mode between compound 34 and c-Met kinase through molecular docking.

Keywords

4-Oxoquinoline; Anti-proliferative activity; Pyrrolo[2,3-b]pyridine derivatives; Synthesis; c-Met.

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