2. Academic Validation
  3. Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents

Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents

  • Bioorg Med Chem Lett. 2021 Feb 1:33:127740. doi: 10.1016/j.bmcl.2020.127740.
Jianqing Zhang 1,  Hehua Xiong 2,  Feiyi Yang 3,  Jie He 3,  Ting Chen 4,  Dongxue Fu 4,  Pengwu Zheng 5,  Qidong Tang 6
Affiliations

Affiliations

  • 1 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China; School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, Jiangxi, China.
  • 2 State Key Laboratory of Natural Medicines, Key Laboratory of Drug Quality Control and Pharmacovigilance, Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
  • 3 School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, Jiangxi, China.
  • 4 The First Affiliated Hospital of Wenzhou Medical University, Wenzhou 325035, China.
  • 5 School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, Jiangxi, China. Electronic address: zhengpw@126.com.
  • 6 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China; School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, Jiangxi, China. Electronic address: tangqidongcn@126.com.
PMID: 33316412 DOI: 10.1016/j.bmcl.2020.127740
Abstract

Cancer is a major cause of death worldwide. Small molecule inhibitors have become a major therapeutic treatment for Cancer. In this study, a series of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives were designed, synthesized and evaluated for their antitumor activity against the A549, Hela and MCF-7 cell lines. Among them, the optimal compound 35 was found to possess excellent inhibitory activity against the A549, Hela and MCF-7 cell lines with IC50 values of 5.29 ± 0.58, 3.72 ± 0.91, and 9.23 ± 0.56 μM, which were superior to Golvatinib. The structure-activity relationship showed that the introduction of 7H-pyrrolo[2,3-d]pyrimidine along with the F atom of the central and terminal benzene was beneficial to the improvement of inhibitory activity of the target compounds. Besides, we took further study on the combined mode between compound 35 and c-Met kinase through molecular docking.

Keywords

4-(Pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide; Antitumor activity; Inhibitors; SAR; Synthesis.

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