二氢吡咯并吡唑类转化生长因子-βⅠ型受体激酶结构域抑制剂：一类对转化生长因子-βⅡ型受体激酶和混合谱系激酶-7具有选择性的新型苯并咪唑系列化合物。
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
作者信息
Li Hong-yu, Wang Yan, Heap Charles R, King Chi-Hsin R, Mundla Sreenivasa R, Voss Matthew, Clawson David K, Yan Lei, Campbell Robert M, Anderson Bryan D, Wagner Jill R, Britt Karen, Lu Ku X, McMillen William T, Yingling Jonathan M
机构信息
Discovery Chemistry Research and Technology, Lilly Research Laboratory, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
出版信息
J Med Chem. 2006 Mar 23;49(6):2138-42. doi: 10.1021/jm058209g.
Novel dihydropyrrolopyrazole-substituted benzimidazoles were synthesized and evaluated in vitro as inhibitors of transforming growth factor-beta type I receptor (TGF-beta RI), TGF-beta RII, and mixed lineage kinase-7 (MLK-7). These compounds were found to be potent TGF-beta RI inhibitors and selective versus TGF-beta RII and MLK-7 kinases. Benzimidazole derivative 8b was active in an in vivo target (TGF-beta RI) inhibition assay.
合成了新型二氢吡咯并吡唑取代的苯并咪唑，并在体外对其作为转化生长因子-β I型受体（TGF-β RI）、TGF-β RII和混合谱系激酶-7（MLK-7）的抑制剂进行了评估。发现这些化合物是有效的TGF-β RI抑制剂，对TGF-β RII和MLK-7激酶具有选择性。苯并咪唑衍生物8b在体内靶点（TGF-β RI）抑制试验中具有活性。
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