Bioisosteric approach to the discovery of imidazo[1,2-a]pyrazines as potent Aurora kinase inhibitors.

Zhaoyang Meng,Bheemashankar A Kulkarni,Angela D Kerekes,Amit K Mandal,Sara J Esposite,David B Belanger,Panduranga Adulla Reddy,Andrea D Basso,Seema Tevar,Kimberly Gray,Jennifer Jones,Elizabeth B Smith,Ronald J Doll,M Arshad Siddiqui

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2011）

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摘要

Our continued effort toward the development of the imidazo[1,2-a] pyrazine scaffold as Aurora kinase inhibitors is described. Bioisosteric approach was applied to optimize the 8-position of the core. Several new potent Aurora A/B dual inhibitors, such as 25k and 25l, were identified. (C) 2010 Elsevier Ltd. All rights reserved.

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关键词

Aurora kinase inhibitors,Imidazo[1,2-a]pyrazine,Bioisosterism

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