Synthesis and Anti-Tumor Activity of Pyridylpyrimidinyl Semicarbazide Derivatives
HU Hong-yu1, JIA Rong1*, ZHAO Sheng-xian2, CAO Ying3, HU Sang-sang1,LI Kun3, YAN Xiao-yang1*
1. Xingzhi College, Zhejiang Normal University, Lanxi 321100, China; 2. College of Science and Technology, Ningbo University, Cixi 315302, China; 3. School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, China
Abstract：OBJECTIVE To design and synthesize N-(4-methyl-3-((4-(pyridin-3-yl) pyrimidin-2-yl) amino) phenyl) hydrazinecarboxamides and investigate their in vitro antitumor activities. METHODS The target compounds were synthesized from N-(2-methyl-5-nitrophenyl)-4-(3-pyridyl)-2-pyrimidine amine through reduction, acylation, hydrazinolysis, and reaction with isocyanates. The synthesized compounds were screened for their anticancer potential against different cancer cells viz human breast (MCF-7) and human hepatoma cell (HepG2) cancer cell lines by MTT assay. RESULTS Thirteen novel compounds were obtained, and their structures were characterized by 1H-NMR, 13C-NMR and HRMS. In vitro bioassay indicated that most compounds showed antitumor activity. Compound 5l displayed the most potential anticancer activity against these cancer cell lines with IC50 value of 9.15 and 10.45 μmol·L-1 respectively, without obvious toxic effects on normal liver cells with IC50 value of 53 μmol·L-1, and it also induced G2/M cell cycle arrest. CONCULUSION The series of compunds show preferable antitumor activities, which are worthy of further study.
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2021, Vol. 56 
