The multicomponent synthesis of a mini-library of histone deacetylase inhibitors with imidazo[1,2-a]pyridine-based cap groups is presented. The biological evaluation led to the discovery of the hit compound MAIP-032 as a selective HDAC6 inhibitor with promising anticancer activity. The X-ray structure of catalytic domain 2 from Danio rerio HDAC6 complexed with MAIP-032 revealed a monodentate zinc-binding mode.

中文翻译：

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咪唑并[1,2 - a ]吡啶封端的选择性HDAC6抑制剂的多组分合成和结合模式

介绍了具有咪唑并[1,2 - a ]吡啶基帽基的组蛋白脱乙酰基酶抑制剂小型文库的多组分合成。生物学评估导致发现了具有抗癌活性的命中化合物MAIP-032，它是一种选择性HDAC6抑制剂。来自丹尼奥雷奥HDAC6与MAIP-032配合的催化域2的X射线结构揭示了单齿锌结合模式。