Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity
作者:Maria Laura Bolognesi、Federica Lizzi、Remo Perozzo、Reto Brun、Andrea Cavalli
DOI:10.1016/j.bmcl.2008.03.009
日期:2008.4
structural features of natural products showing anti-trypanosomatid activity, we designed and synthesized a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives. The library was obtained following a parallel approach and using readily available synthons. All the derivatives showed inhibitory activity toward either Trypanosoma or Leishmania species, with 8, 10, and
利用显示抗锥虫活性的天然产物的结构特征,我们设计并合成了一个小的2-苯氧基-1,4-萘醌和2-苯氧基-1,4-蒽醌衍生物文库。该文库是通过并行方法并使用容易获得的合成子获得的。所有衍生物均对锥虫或利什曼原虫种均显示抑制活性,其中8、10和16是对布鲁氏锥虫,杜氏利什曼原虫和克鲁氏锥虫细胞最具活性的化合物(IC(50)= 50nM,IC(50)=分别为0.28 microM和IC(50)= 1.26 microM)。