DiSCAFF, Università degli Studi del Piemonte Orientale, via Bovio 6, 28100, Novara, Italy.
Org Biomol Chem. 2011 Jun 7;9(11):4144-9. doi: 10.1039/c1ob05336a. Epub 2011 Apr 14.
In a program aimed at discovering novel protein kinase inhibitors, a convenient synthesis of 3,8-diaminoimidazo[1,2-a]pyrazines has been developed exploiting the isocyanide-based multicomponent Blackburn reaction, followed by a nucleophilic aromatic substitution with ammonia or primary and secondary amines. The potential of the reported scaffold is strengthened by the inhibition of STAT5-dependent transcription displayed by four of the synthesized compounds.
在一个旨在发现新型蛋白激酶抑制剂的项目中，利用基于异氰化物的多组分 Blackburn 反应，随后与氨或伯胺和仲胺进行亲核芳香取代，开发了一种方便的 3,8-二氨基咪唑并[1,2-a]吡嗪合成方法。所报道的支架的潜力通过四种合成化合物对 STAT5 依赖性转录的抑制得到了加强。
