2. Academic Validation
  3. Discovery of novel 2-substituted-4-phenoxypyridine derivatives as potential antitumor agents

Discovery of novel 2-substituted-4-phenoxypyridine derivatives as potential antitumor agents

  • Bioorg Med Chem Lett. 2018 Feb 1;28(3):254-259. doi: 10.1016/j.bmcl.2017.12.063.
Yongli Duan 1,  Shan Xu 1,  Hehua Xiong 1,  Linxiao Wang 1,  Bingbing Zhao 1,  Ping Wang 1,  Caolin Wang 1,  Yiqing Peng 1,  Shifan Cai 1,  Rong Luo 2,  Pengwu Zheng 3,  Qidong Tang 4
Affiliations

Affiliations

  • 1 Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China.
  • 2 Jiangxi Province Institute of Materia Medica, Nanchang 330000, PR China.
  • 3 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.
  • 4 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: 29317165 DOI: 10.1016/j.bmcl.2017.12.063
Abstract

A series of 2-substituted-4-phenoxypyridine derivatives were designed, synthesized, and evaluated for their antiproliferative activity against 4 Cancer cell lines (A549, HT-29, H460, and U87MG) in vitro. Most compounds showed moderate to excellent potency. Nine tyrosine kinases (c-Met, Flt-3, ALK, VEGFR-2, VEGFR-3, PDGFR-α, PDGFR-β, c-Kit, and EGFR) were used to evaluate the inhibitory activities with the most promising analogue 39, which showed the Flt-3/c-Met IC50 values of 2.18/2.61 nM. Structure-activity relationship studies indicated that n-Pr served as R1 group showed a higher preference, and stronger mono-EWGs on the phenyl ring (such as R2 = 4-F) was benefited to the potency.

Keywords

1,8-Naphthyridinone; 4-Phenoxypyridine derivatives; Antiproliferative activity; Flt-3; Synthesis; c-Met.

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