Journal of Medicinal Chemistry p. 775 - 781 (1990)
Update date:2022-08-04
Topics:
Yamashita
Schaub
Back
White
Toy
Ghazal
Burdick
Brashler
Holm
A series of substituted 1,4-dihydronaphthoquinones, hydroindoloquinones, benzofuran-4,7-dihydroquinones, and benzothiophene-4,7-dihydroquinones were synthesized and evaluated for inhibitory activity against 5-lipoxygenase. These compounds were found to be active in vitro for LTC4/D4 inhibition with the potencies (IC50's) ranging from 0.2 to 85 μM. Active 1,4-dihydronaphthoquinone acetates (IC50 < 20 μM) were evaluated in an ex vivo LTB4 inhibition assay. The acetates of 1,4-dihydronaphthoquinones containing the alkyl substituent(s) (2-n-butyl, 11, and 2,3-diethyl, 15) exhibited the best activity in LTC4/D4 inhibition (IC50 = 0.2-0.4 μM, in vitro) as well as in LTB4 inhibition (60-75% inhibition).
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