Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
作者： Joan Carboni , Aixin Li , Ann Greer , Marco Gottardis , Ricardo M. Attar
DOI: 10.1016/J.BMCL.2008.05.104
关键词:
摘要: 3-(Benzimidazol-2-yl)-pyridine-2-one-based ATP competitive inhibitors of Insulin-like Growth Factor 1 Kinase (IGF-IR) were optimized for reduced Cyp3A4 inhibition and improved oral exposure. The use malonate as methyl anion synthon via S N Ar reaction double decarboxylation under mild conditions is demonstrated.
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