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 e valuate their ability to inhibit Protein Kinase C (PKC) activation. Th e model consisted in the detection of the superoxide anion in activate d neutrophils. Naphthopyrans carrying 3-(diethylamino), 3-(1-piperidin yl) 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 wit h an increase in anti-PKC activity. No activity was found when an elec tron withdrawing group was placed in position 2 of the 3-(dialkylamino )-1H-naphtho [2,1-b] pyran-1-ones.