Design, synthesis and antitumor activity evaluation of 5-cyano-2,4,6-substituted pyrimidine derivatives containing acrylamide group

  • Impact factors: 2.6
  • Publication: MEDICINAL CHEMISTRY RESEARCH
  • Author:Yu Fuqiang,Chi Lingling,Wang Hao,Gao Chao,Dai Honglin,Liu Limin,Wang Zhengjie,Ke Yu,Liu Hongmin,Zhang Qiurong
  • DOI citation-doi:10.1007/s00044-023-03099-7
  • Date:2023-07-07

A series of novel 5-cyano-2,4,6-substituted pyrimidine derivatives containing acrylamide group were designed, synthesized, and evaluated for their antitumor activity against four human cancer cell lines (MGC-803, PC-3, A549, and H1975) using the MTT assay. Among them, compound 20y exhibited the most potent cytotoxicity against PC-3 cells (IC 50  = 2.75 ± 0.08 μM). Notably, compound 20y significantly inhibited the colony formation, migration, and invasion of PC-3 cells. Furthermore, compound 20y induced S-phase cell cycle arrest and apoptosis in PC-3 cells. These findings indicate that compound 20y might serve as a valuable lead compound for developing antitumor agents targeting prostate cancer cells. Graphical Abstract

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