当前位置:
X-MOL 学术
›
Bioorg. Med. Chem. Lett.
›
论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
AZD5597的发现,一种有效的咪唑嘧啶酰胺CDK抑制剂,适合静脉内给药。
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2008 Dec 15 , DOI: 10.1016/j.bmcl.2008.10.102 Clifford D. Jones , David M. Andrews , Andrew J. Barker , Kevin Blades , Paula Daunt , Simon East , Catherine Geh , Mark A. Graham , Keith M. Johnson , Sarah A. Loddick , Heather M. McFarland , Alexandra McGregor , Louise Moss , David A. Rudge , Peter B. Simpson , Michael L. Swain , Kin Y. Tam , Julie A. Tucker , Mike Walker
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2008 Dec 15 , DOI: 10.1016/j.bmcl.2008.10.102 Clifford D. Jones , David M. Andrews , Andrew J. Barker , Kevin Blades , Paula Daunt , Simon East , Catherine Geh , Mark A. Graham , Keith M. Johnson , Sarah A. Loddick , Heather M. McFarland , Alexandra McGregor , Louise Moss , David A. Rudge , Peter B. Simpson , Michael L. Swain , Kin Y. Tam , Julie A. Tucker , Mike Walker
描述了开发新型系列的咪唑嘧啶酰胺作为细胞周期蛋白依赖性激酶(CDK)抑制剂。对多种CDK(1、2和9)的抑制效能的优化导致了咪唑嘧啶酰胺具有针对多种癌细胞的有效体外抗增殖作用。通过改变亲脂性和胺碱性,获得了优异的理化特性和对CYP亚型和hERG离子通道的抑制作用。选择具有人癌细胞系异种移植物中的疾病模型活性并且具有适合静脉内(iv)剂量的理化和药代动力学特征的候选人作为AZD5597进行进一步开发。
"点击查看英文标题和摘要"
更新日期:2017-01-31
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
"点击查看英文标题和摘要"