嘧啶类细胞周期蛋白依赖性激酶抑制剂的研究进展.pdfVIP

中国科技论文在线 嘧啶类细胞周期蛋白依赖性激酶抑制剂的 # 研究进展 赵培亮，游文玮* 5 （南方医科大学药学院化学系，广州，510515 ） 摘要： 嘧啶类化合物因其广泛的生物活性在医药、农药等领域备受关注，特别是近年来大 量具有抗肿瘤活性的嘧啶类细胞周期蛋白依赖性激酶(CDKs)抑制剂被报道，其中一些化合 物已进入临床试验阶段。本文根据化合物结构的特点，将具有细胞周期蛋白依赖性激酶抑 制活性的嘧啶类化合物归纳为2-位含氨基嘧啶类、4-位含氨基嘧啶类、2,4-二位含氨基嘧啶 10 类和稠环类嘧啶化合物，介绍其在抗肿瘤药物研究中的最新进展。 关键词：嘧啶; 细胞周期蛋白依赖性激酶；研究进展 中图分类号：O62 Research advances in cyclin-dependent kinases inhibition of 15 pyrimidine derivatives ZHAO Peiliang, YOU Wenwei (Department of Chemistry, School of Pharmaceutical Science, Southern Medical University, Guangzhou 510515, PR China) Abstract: Pyrimidines are important active structures in medicine and agrochemical fields. 20 Particularly, a large number of these compounds have recently been reported to show substantial inhibition of cyclin-dependent kinases, and some of them have been investigated in clinical trials. In this paper, inhibitions of cyclin-dependent kinases of pyrimidine derivatives were briefly reviewed, which were classified into 2-amines, 4-amines, 2,4-diamines and fused rings according to the structure features ． 25 Key words: pyrimidine; cyclin-dependent kinases inhibition; research advances 0 引言 细胞周期指细胞分裂的时相变化，即从细胞分裂结束开始，到下一次细胞分裂结束为止 的过程，是细胞生命活动的基本过程。细胞在进化过程中发展并建立了一系列的调控机制， 30 这些调控机制确保细胞周期严格有序的交替和各时相依次有序变更[1-4] 。而细胞周期蛋白依