酯瓜氨酸类似物的合成及其对磷脂酰肌醇4-激酶的抑制活性。

Y Saito, K Kato, K Umezawa
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引用次数: 3

摘要

制备了n -取代-2-氨基-4(3H)- 7h -氧基吡啶[2,3-d]嘧啶-5-碳酰胺及其核呋喃基和2',3'-二脱氧核呋喃基衍生物作为膜透性乙酰瓜氨酸类似物,并测试了它们抑制磷脂酰肌醇(PI) 4激酶的能力。乙胺5和相应的核呋喃基化合物11抑制PI 4-激酶的IC50值分别为0.02和2.4微克/毫升。
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Synthesis and inhibitory activity against phosphatidylinositol 4-kinase of echiguanine analogs.

N-Substituted-2-amino-4(3H)-7H-oxopyrrolo[2,3-d]pyrimidine-5-carbo xamides and their ribofuranosyl and 2',3'-dideoxyribofuranosyl derivatives were prepared as membrane permeable echiguanine analogs and tested for their ability to inhibit phosphatidylinositol (PI) 4-kinase. The ethylamide 5 and the corresponding ribofuranosyl compound 11 inhibited PI 4-kinase with IC50 values of 0.02 and 2.4 micrograms/ml, respectively.

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