Replacement of one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 (1) with sulfonamide containing substituents produced a new class of active and potent PI3Kα inhibitors. Solubility issues prevented all but the 6-amino derivative 17 from being evaluated in vivo, but the clear activity of this compound demonstrated that this class of PI3K inhibitor shows great promise.

中文翻译：

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磷脂酰肌醇3-激酶抑制剂ZSTK474的磺酰胺类似物的合成及生物学评价

磷脂酰肌醇3-激酶（PI3K）抑制剂ZSTK474（1）的一个吗啉基团被含磺酰胺的取代基取代产生了新型的活性和有效PI3Kα抑制剂。溶解度问题阻止了除6-氨基衍生物17以外的所有化合物在体内的评估，但该化合物的明显活性表明此类PI3K抑制剂具有广阔的前景。