Müller K, Reindl H, Breu K
Institut für Pharmazeutische Chemie, Westfälische Wilhelms-Universität Münster, Germany.
Bioorg Med Chem Lett. 2001 Jan 8;11(1):47-50. doi: 10.1016/s0960-894x(00)00599-0.
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.
合成了抗银屑病药物蒽林的杂环取代衍生物，并在体外评估了它们对角质形成细胞的抗增殖作用以及诱导角质形成细胞分化的能力。吲哚 -2- 羧酸类似物 2e 表现出与蒽林相同的优异抗增殖活性，还能诱导角质形成细胞的终末分化。由于其产生氧自由基的潜力大大降低，2e 不会诱导角质形成细胞膜的损伤。
