title: Heterocyclic substituted anthralin derivatives as inhibitors of keratinocyte growth and inducers of differentiation.
abstract: Heterocyclic substituted derivatives of the antipsoriatic anthralin were synthesized and evaluated in vitro for their antiproliferative action against keratinocytes and their ability to induce keratinocyte differentiation. The indole-2-carboxylic acid analogue 2e exhibited the same excellent antiproliferative activity as anthralin and also induced terminal differentiation of keratinocytes. As a benefit of its strongly diminished potential to generate oxygen radicals, 2e did not induce damage of keratinocyte membranes.
authors.affiliation: Institut für Pharmazeutische Chemie, Westfälische Wilhelms-Universität Münster, Germany. kmuller@uni-muenster.de
authors.forename: K
authors.initials: K
authors.lastname: Müller
authors.forename: H
authors.initials: H
authors.lastname: Reindl
authors.forename: K
authors.initials: K
authors.lastname: Breu
mesh_terms: D000287:Administration, Topical; D000875:Anthralin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D002454:Cell Differentiation / Q000187:drug effects*; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D003855:Deoxyribose / Q000378:metabolism; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D015603:Keratinocytes / Q000166:cytology* / Q000187:drug effects*; D015394:Molecular Structure; D011565:Psoriasis / Q000188:drug therapy
chemical_list: D000893:Anti-Inflammatory Agents; D006571:Heterocyclic Compounds; D003855:Deoxyribose; D000875:Anthralin