Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.
Eur J Med Chem. 2010 Apr;45(4):1424-9. doi: 10.1016/j.ejmech.2009.12.046. Epub 2009 Dec 28.
A series of novel chalconoids containing a 6-chloro-2H-chromen-3-yl group were prepared through a convenient and efficient synthetic method by using 5-chloro-2-hydroxybenzaldehyde as starting material. The target compounds were evaluated against the promastigote form of Leishmania major using MTT assay. All of the evaluated compounds have shown high in vitro antileishmanial activity at concentrations less than 3.0 microM. The results of cytotoxicity assessment against mouse peritoneal macrophage cells showed that these compounds display antileishmanial activity at non-cytotoxic concentrations.
一系列含有 6-氯-2H-色烯-3-基的新型查耳酮类化合物通过一种简便高效的合成方法制备，以 5-氯-2-羟基苯甲醛为起始原料。采用 MTT 法测定了目标化合物对利什曼原虫前鞭毛体的活性。所有评价的化合物在低于 3.0μM 的浓度下均表现出很高的体外抗利什曼原虫活性。对小鼠腹腔巨噬细胞的细胞毒性评估结果表明，这些化合物在非细胞毒性浓度下具有抗利什曼原虫活性。
