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摘要:Cancer is a leading cause of death worldwide,the development of new drugs that are safe and efficient has been one of the biggest challenges in combating cancer[1] Nowadays,numerous studies have been made to show the biological significance of different pyrimidine derivative[2].Pyrimidine moiety is one of the essential classes of N-containing heterocycles and extensively used as key building blocks for pharmaceutical agents[3].In this paper,we used 4,4,4-trifluoromethylacetoacetate and thiourea as starting materials and obtained a series of novel 2,4,6-substituted pyrimidine derivatives through cyclization and substitution reactions.All the compounds have been confirmed by 1 H-NMR,13C-NMR and MS.Currently,we evaluated for their antitumor activities by using MTT assay in vitro.Especially compound 4 g {N-((4-ethylphenyl)carbamoyl)-2-((4-((4-methoxvphenyl)amino)-6-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide} had good anti-tumor activity against SW-620 with IC50 value of1.46 μM which was better than 5-fluorouracil(10.32 μM).
会议名称:

第11届世界华人药物化学研讨会(ISCMC 2018)

会议时间:

2018-08-24

会议地点:

中国河南郑州

  • 专辑:

    医药卫生

  • 专题:

    药学; 药学

  • 分类号:

    R914;R96

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