10-omega-phenylalkyl-9(10H)-anthracenones as inhibitors of keratinocyte growth with reduced membrane damaging properties.
Work aimed at further improving the benefit to risk ratio of the antipsoriatic agent anthralin has led to 10-omega-phenylalkyl-9(10H)-anthracenones, members of which are equally potent as inhibitors of the growth of HaCaT keratinocytes. In contrast to anthralin, induction of membrane injury is strongly reduced as documented by the release of LDH activity from cytoplasm of keratinocytes.
Müller
K
K
Institut für Pharmazeutische Chemie, Westfälische Wilhelms-Universität Münster, Germany. kmuller@uni-muenster.de
Breu
K
K
D000287:Administration, Topical; D000875:Anthralin / Q000031:analogs & derivatives*; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002462:Cell Membrane / Q000187:drug effects; D006131:Growth Inhibitors / Q000494:pharmacology*; D006801:Humans; D017665:Hydroxyl Radical; D015603:Keratinocytes / Q000187:drug effects*; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D011565:Psoriasis / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000893:Anti-Inflammatory Agents; D006131:Growth Inhibitors; D017665:Hydroxyl Radical; D007770:L-Lactate Dehydrogenase; D000875:Anthralin