新型咪唑并[1,2-a]吡啶类 IGF-1 受体酪氨酸激酶抑制剂的研究：苯胺基的优化。
Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.
机构信息
AstraZeneca, Oncology Innovative Medicines, Centre de recherches, Z.I. Pompelle, 51689 Reims Cedex 2, France.
出版信息
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4702-4. doi: 10.1016/j.bmcl.2011.06.090. Epub 2011 Jun 25.
PMID:21764307
Abstract
Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure-activity relationships against IGF-1R kinase activity as well as inhibition of the hERG ion channel are discussed.
摘要
继发现咪唑并吡啶 1 作为一种有效的 IGF-1R 酪氨酸激酶抑制剂后，本研究对苯胺部分进行了修饰，旨在优化该系列化合物的性质。本文讨论了其对 IGF-1R 激酶活性的构效关系以及对 hERG 离子通道的抑制作用。
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