Synthesis and Inhibitory Activity Against Phosphatidylinositol 4-Kinase of Echiguanine Analogs |
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| Authors: | Yoshio Saito Kuniki Kato Kazuo Umezawa |
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| Institution: | 1. Department of Applied Chemistry, Faculty of Science and Technology , Keio University , 3-14-1 Hiyoshi Kohoku-ku, Yokohama, 223-0061, Japan;2. Research Laboratories, Pharmaceuticals Group , Nippon Kayaku Co. Ltd. , 3-31 Shimo, Kita-ku, Tokyo, 115-0042, Japan |
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| Abstract: | Abstract N-Substituted-2-amino-4(3H)-7H-oxopyrrolo2,3-d]pyrimidine-5-carboxamides 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 μg/ml, respectively. |
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