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Synthesis and structure-activity relationship of ribofuranosyl echiguanine analogs as inhibitors of phosphatidylinositol 4-kinase

✍ Scribed by Yoshio Saito; Kuniki Kato; Kazuo Umezawa

Book ID
104208497
Publisher
Elsevier Science
Year
1998
Tongue
French
Weight
923 KB
Volume
54
Category
Article
ISSN
0040-4020

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✦ Synopsis

N-Substituted-2-amino-4(3/-/)-7H-oxopyrrolo[2,3-d]pyrimidine-5-carboxamides and their ribofuranosyl and 2',3'-dideoxyribofuranosyl derivatives were ixcpared as membrane permeable ¢chiguanine analogs and tested for their ability to inhibit phosphatidylinositol (PI) 4-kinase. Compounds 5 and 6 were found to inhibit the enzyme approximately at the same level as echiguanines A and B.

It is noteworthy that ribofuranosides 18, 19, and 20 and didcoxyribofuranosid¢ 29 effectively inhibited PI 4-kinase. Thus, the terminal amide and relamd structures may be preferable for inhibition of the enzyme in echiguanine analogs with or without ribofuranosidc.

📜 SIMILAR VOLUMES

Synthesis of ribofuranosyl glycosides of
Synthesis of ribofuranosyl glycosides of echiguanines A and B, inhibitors of phosphatidylinositol 4-kinase
✍ Kasumi Sanpei; Yoshio Saito; Masaya Imoto; Kazuo Umezawa; Kuniki Kato 📂 Article 📅 1996 🏛 Elsevier Science 🌐 English ⚖ 195 KB

The synthesis of ribofuranosyl glycosides of echiguanines A and B, PI 4-kinase inhibitors, was achieved from 2-amino-4-chloropyrrolo[2,3-d]pyrimidine and 2,3-O-isopropylidene-5-O-(t-butyl) dimethylsilyl-o~-D-ribofuranosyl chloride. The ribofuranosyl echiguanine A weakly inhibited PI 4-kinase.