Selective and novel cyclin-dependent kinases 4 inhibitor: synthesis and biological evaluation
Selective and novel cyclin-dependent kinases 4 inhibitor: synthesis and biological evaluation
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选择性和新型细胞周期蛋白依赖性激酶 4 抑制剂：合成和生物学评价
DOI：
10.1007/s00044-018-2180-2
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发表时间：
2018-04
影响因子：
2.6
通讯作者：
Fan Y
中科院分区：
文献类型：
--
作者：
Guo Qingxiang;Li Yongtao;Zhang Chao;Huang Zhi;Wang Xin;Nie Yongwei;Li Yao;Liu Yanhua;Xiang Rong;Fan Yan;Yang Shengyong;Xiang Rong;Fan Yan;Xiang R;Fan Y;Xiang R;Fan Y
设计、合成并评估了一系列含吡啶 N - 氧化物的新型LEE011衍生物。对构效关系（SAR）的系统研究提高了对细胞周期蛋白依赖性激酶4（CDK4）的选择性，并确定了化合物9a。该……
（原文“the co”不完整，可能影响完整理解，以上翻译基于已有内容。）
A series of novel LEE011 derivatives containing pyridine N-oxide were designed, synthesized and evaluated. Systematic study of the structure-activity relationship (SAR) improves the selectivity for CDK4 and led to the identification of compound9a. The compound showed comparable CDK4 kinase activity with ribociclib and greater selectivity over the closely related CDK6 kinase. The selective CDK4 inhibitor9ahas been demonstrated the antitumor activity via G1 phase cell cycle arrest, as well as dual CDK4/CDK6 inhibitor ribociclib and significantly down-regulated the activity of CDK4-cyclinD-Rb pathway of tumor cells. Taken together, this compound may act as promising lead compound for further development of new CDK4 inhibitors.
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影响因子：
3.1
作者：
B. Saikia;Rajiv Khatioda;Pranita Bora;B. Sarma
通讯作者：
B. Saikia;Rajiv Khatioda;Pranita Bora;B. Sarma
影响因子：
64.8
作者：
Antony J. Michalski
通讯作者：
Antony J. Michalski
影响因子：
--
作者：
A. Kamal;V. S. Reddy;K. Santosh;Gajjela Bharath Kumar;A. B. Shaik;R. Mahesh;Sumit Chourasiya;I. Sayeed;S. Kotamraju
通讯作者：
A. Kamal;V. S. Reddy;K. Santosh;Gajjela Bharath Kumar;A. B. Shaik;R. Mahesh;Sumit Chourasiya;I. Sayeed;S. Kotamraju
影响因子：
5.7
作者：
Chen, Ping;Lee, Nathan V.;Murray, Brion W.
通讯作者：
Murray, Brion W.
影响因子：
2.7
作者：
Sanchez-Martinez, Concepcion;Gelbert, Lawrence M.;de Dios, Alfonso
通讯作者：
de Dios, Alfonso