Krebs A, Schaltegger H, Schaltegger A
Br J Dermatol. 1981 Aug;105 Suppl 20:6-11. doi: 10.1111/j.1365-2133.1981.tb00990.x.
In the investigations of Krebs and Schaltegger between 1964 and 1972 on the structure specificity of the antipsoriatic anthrones it could be shown that at least a 1-hydroxy-9-anthrone is necessary for their efficacy. This structure was then called "minimum structure of the antipsoriatic anthrones'. Since even very minor changes of this structure in most cases lead to inactive compounds, only a few antipsoriatic anthrones have been found so far. Their most important representative chrysarobin, anthralin and I-hydroxy-9-anthrone have been known for more than 60 years. The later discovered antipsoriatic anthralin derivatives, triacetoxy-anthracene and 10-acyl-anthralin, are probably hydrolysed in the skin and thus act as their parent compound anthralin. The strong structure-activity dependence of the antipsoriatic anthrones seems to include a highly specific and complex mechanism of action.
在1964年至1972年间，克雷布斯和沙尔特格对治疗银屑病的蒽酮类药物的结构特异性进行了研究，结果表明，至少1-羟基-9-蒽酮对其疗效是必需的。这种结构随后被称为“治疗银屑病蒽酮类药物的最小结构”。由于在大多数情况下，即使这种结构发生非常微小的变化也会导致化合物失去活性，所以到目前为止只发现了少数几种治疗银屑病的蒽酮类药物。它们最重要的代表药物柯桠素、蒽林和1-羟基-9-蒽酮已经被人们所知超过60年了。后来发现的治疗银屑病的蒽林衍生物，三乙酰氧基蒽和10-酰基蒽林，可能在皮肤中被水解，从而以其母体化合物蒽林的形式发挥作用。治疗银屑病的蒽酮类药物对结构-活性的强烈依赖性似乎包括一种高度特异性和复杂的作用机制。
