新型3-烷氧基-1H-吡唑并[3,4-d]嘧啶作为表皮生长因子受体（EGFR）和erbB2受体酪氨酸激酶抑制剂
Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.
作者信息
Ducray Richard, Ballard Peter, Barlaam Bernard C, Hickinson Mark D, Kettle Jason G, Ogilvie Donald J, Trigwell Catherine B
机构信息
AstraZeneca, Centre de Recherches, Z.I. la Pompelle, BP1050, 51689 Reims Cedex 2, France.
出版信息
Bioorg Med Chem Lett. 2008 Feb 1;18(3):959-62. doi: 10.1016/j.bmcl.2007.12.035. Epub 2007 Dec 23.
PMID:18182285
Abstract
Novel 4-anilino-1H-pyrazolo[3,4-d]pyrimidines have been synthesized and evaluated in vitro for erbB2 and EGFR kinase inhibition. A representative compound displaying oral bioavailability in rat and dog illustrates the potential of this series to provide orally active erbB2 inhibitors.
摘要
新型4-苯胺基-1H-吡唑并[3,4-d]嘧啶已被合成，并在体外评估其对erbB2和EGFR激酶的抑制作用。一种在大鼠和犬中显示出口服生物利用度的代表性化合物表明了该系列提供口服活性erbB2抑制剂的潜力。
Zotero 插件