Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable
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- 作者：David Buttar ; Mike Edge ; Steve C. Emery ; Martina Fitzek ; Cheryl Forder ; Alison Griffen ; Barry Hayter ; Chris F. Hayward ; Philip J. Hopcroft ; Richard W.A. Luke ; Ken Page ; John Stawpert ; Andy Wright
- 关键词：Angiogenesis ; Kinase ; Tie-2 ; Inhibitor ; Pyrimidine ; Imidazole ; Alkene
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 August 2008
- 年：2008
- 卷：18
- 期：16
- 页码：4723-4726
- 全文大小：248 K
文摘
Tie-2 is a receptor tyrosine kinase which is involved in angiogenesis and thereby growth of human tumours. The discovery and SAR of a novel class of imidazole-vinyl-pyrimidine kinase inhibitors, which inhibit Tie-2 in vitro is reported. Their synthesis was carried out by condensation of imidazole aldehydes with methyl pyrimidines. These compounds are lead-like, with low molecular weight, good physical properties and oral bioavailability.