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.
Saito
Y
Y
Department of Applied Chemistry, Faculty of Science and Technology, Keio University, Yokohama, Japan.
Kato
K
K
Umezawa
K
K
D019870:1-Phosphatidylinositol 4-Kinase / Q000037:antagonists & inhibitors*; D006147:Guanine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D006147:Guanine; D019870:1-Phosphatidylinositol 4-Kinase