2002 enzyme inhibiting activity

enzyme inhibiting activityX 0220

01 - 2541-Arylalkyl-Substituted Anthracenones as Inhibitors of 12-Lipoxygenase Enzymes. Part 1. Structure–Activity Relationships ofthe Terminal Aryl Ring. — Twenty-five anthracenones are synthesizedand tested as inhibitors of three types of 12-lipoxygenase isoforms. Selective in-hibition of 12-lipoxygenase enzymes is dependent on a high overall lipophilicity,otherwise the compounds are also able to inhibit the 5-LO enzyme. Althoughpotent inhibitors can be identified (e.g. (Ic)), these agents are not usefulas potentially selective inhibitors. Anthracenones (Ia) and (Ib) are selectiveinhibitors of the platelet-type 12-LO isoform, but none of the compounds isable to discriminate between the epidermal-type and the other-LO isoforms.— (MUELLER, KLAUS; ALTMANN, REINHOLD; PRINZ, HELGE; Eur. J.Med. Chem. 36 (2001) 6, 569-575; Inst. Pharm. Chem., Westfael. Wilhelms-Univ., D-48149 Muenster, Germany; EN)

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