Oliveira João, Ralton Lynda, Tavares Joana, Codeiro-da-Silva Anabela, Bestwick Charles S, McPherson Anne, Thoo Lin Paul Kong
The Robert Gordon University, School of Life Sciences, St. Andrew Street, Aberdeen AB25 1HG, Scotland, UK.
Bioorg Med Chem. 2007 Jan 1;15(1):541-5. doi: 10.1016/j.bmc.2006.09.031. Epub 2006 Sep 28.
Bisnaphthalimidopropyl derivatives (BNIPSpd, BNIPDaoct, BNIPDanon, BNIPDadec, BNIPDpta and BNIPDeta) were synthesised in yields ranging from 50% to 70% and their cytotoxicity against colon cancer cells (Caco-2) and the parasite Leishmania infantum determined using the MTT assay. Cytotoxicity within Caco-2 cells was manifested with IC(50) values between 0.3 and 22 microM. Compounds with the central longer alkyl chains exhibited the highest cytotoxicity. Against L. infantum, IC(50) values were encompassed within a narrower concentration range of 0.47-1.54 microM. In the parasites, the presence of nitrogen in the central chain and the length of the central alkyl chains did not especially enhance cytotoxicity. This may be due to the way these compounds are transported in the cells.
合成了双萘二甲酰亚胺丙基衍生物（BNIPSpd、BNIPDaoct、BNIPDanon、BNIPDadec、BNIPDpta和BNIPDeta），产率在50%至70%之间，并使用MTT法测定了它们对结肠癌细胞（Caco-2）和寄生虫婴儿利什曼原虫的细胞毒性。Caco-2细胞内的细胞毒性表现为IC(50)值在0.3至22微摩尔之间。具有较长中心烷基链的化合物表现出最高的细胞毒性。对于婴儿利什曼原虫，IC(50)值涵盖在0.47 - 1.54微摩尔的较窄浓度范围内。在寄生虫中，中心链中氮的存在和中心烷基链的长度并没有特别增强细胞毒性。这可能是由于这些化合物在细胞内的运输方式所致。
