A synthesis of 2-substituted 2-aminoethanol derivatives having inhibitory activity against protein kinase C.
A series of 2-aminoethanol derivatives was synthesized and their inhibitory activities against protein kinase C were investigated. Among these compounds, 2-endo-hexadecylamino-5-norbornene-2- exo-methanol (4h) and 2-endo-hexadecylamino-5-norbornene-2,3-exo-dimethanol (4i) inhibited protein kinase C at the IC50 values of 2 x 10(-5) and 1 x 10(-5) M, respectively, but not protein kinase A at a concentration of 1 x 10(-3) M. The structure-activity relationships are discussed.
Iwasaki
T
T
Research Laboratory of Applied Biochemistry, Tanabe Seiyaku Co., Ltd., Osaka, Japan.
Yamazaki
H
H
Nishitani
T
T
Kondo
K
K
Sato
T
T
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology; D002417:Cattle; D004983:Ethanolamines / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D009636:Norbornanes / Q000138:chemical synthesis / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D051381:Rats
D004983:Ethanolamines; D009636:Norbornanes; D011493:Protein Kinase C