新型嘧啶并[4,5-d]嘧啶 CDK2 抑制剂作为抗肿瘤药物的设计、合成及生物学评价
Design, Synthesis and Biological Evaluation of Novel Pyrimido[4,5-d]pyrimidine CDK2 Inhibitors as Anti-Tumor Agents.
作者信息
El-Moghazy Samir M, Ibrahim Diaa A, Abdelgawad Nagwa M, Farag Nahla A H, El-Khouly Ahmad S
机构信息
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
出版信息
Sci Pharm. 2011 Jul-Sep;79(3):429-47. doi: 10.3797/scipharm.1103-16. Epub 2011 May 8.
A series of 2,5,7-trisubstituted pyrimido[4,5-d]pyrimidine cyclin-dependent kinase (CDK2) inhibitors is designed and synthesized. 6-Amino-2-thiouracil is reacted with an aldehyde and thiourea to prepare the pyrimido[4,5-d]-pyrimidines. Alkylation and amination of the latter ones give different amino derivatives. These compounds show potent and selective CDK inhibitory activities and inhibit in vitro cellular proliferation in cultured human tumor cells.
设计并合成了一系列2,5,7-三取代嘧啶并[4,5-d]嘧啶细胞周期蛋白依赖性激酶（CDK2）抑制剂。6-氨基-2-硫脲与醛和硫脲反应制备嘧啶并[4,5-d]嘧啶。后者的烷基化和胺化反应得到不同的氨基衍生物。这些化合物表现出强效且选择性的CDK抑制活性，并能抑制培养的人肿瘤细胞的体外细胞增殖。
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