3-(1H-苯并[d]咪唑-2-基)吡啶-2(1H)-酮类胰岛素样生长因子受体-1（IGF-1R）抑制剂中咪唑部分的取代，以改善细胞色素P450特性。
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.
作者信息
Velaparthi Upender, Liu Peiying, Balasubramanian Balu, Carboni Joan, Attar Ricardo, Gottardis Marco, Li Aixin, Greer Ann, Zoeckler Mary, Wittman Mark D, Vyas Dolatrai
机构信息
Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3072-6. doi: 10.1016/j.bmcl.2007.03.048. Epub 2007 Mar 19.
A series of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) were examined in which the pendant imidazole moiety was replaced to improve selectivity for IGF-1R inhibition over cytochrome P450 (CYP). Synthesis and SAR of these compounds is presented.
研究了一系列胰岛素样生长因子受体-1（IGF-1R）的3-（1H-苯并[d]咪唑-2-基）吡啶-2（1H）-酮抑制剂，其中侧链咪唑部分被取代以提高对IGF-1R的抑制选择性，优于细胞色素P450（CYP）。介绍了这些化合物的合成及构效关系。
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