Heterocyclic substituted anthralin derivatives as inhibitors of keratinocyte growth and inducers of differentiation

Heterocyclic substituted derivatives of the antipsoriatic anthralin were sy nthesized and evaluated in vitro for their antiproliferative action against keratinocytes and their ability to induce keratinocyte differentiation. Th e indole-2-carboxylic acid analogue 2e exhibited the same excellent antipro liferative activity as anthralin and also induced terminal differentiation of keratinocytes. As a benefit of its strongly diminished potential to gene rate oxygen radicals, 2e did not induce damage of keratinocyte membranes. ( C) 2000 Elsevier Science Ltd. All rights reserved.