Anti-PKC activity of some 3-(dialkylamino)-1H-naphtho [2,1-B] pyran-1-ones.
Some 3-(dialkylamino)-1H-naphtho [2,1-b] pyran-1-ones were tested to evaluate their ability to inhibit Protein Kinase C (PKC) activation. The model consisted in the detection of the superoxide anion in activated neutrophils. Naphthopyrans carrying 3-(diethylamino), 3-(1-piperidinyl) and 3-[bis(2-methoxyethyl)amino] groups emerged as the most active ones. Introduction of alkoxy groups in position 8 and 9 and of bromo substituent in position 8 on the naphthalene moiety was associated with an increase in anti-PKC activity. No activity was found when an electron withdrawing group was placed in position 2 of the 3-(dialkylamino)-1H-naphtho [2,1-b] pyran-1-ones.
Mazzei
M
M
Istituto di Chimica Biologica, Genova.
Garzoglio
R
R
Sottofattori
E
E
Melloni
E
E
Michetti
M
M
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D008262:Macrophage Activation / Q000187:drug effects; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D011753:Pyrones / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013481:Superoxides / Q000378:metabolism
D004791:Enzyme Inhibitors; D009281:Naphthalenes; D011753:Pyrones; D013481:Superoxides; D011493:Protein Kinase C