Synthesis, cytotoxicity and structure-activity relationships between ester and amide functionalities in novel acridine-based platinum(II) complexes
作者:Florence Bouyer、Johnny Moretto、David Pertuit、Anna Szollosi、Marie-Aleth Lacaille-Dubois、Yves Blache、Bruno Chauffert、Nicolas Desbois
DOI:10.1016/j.jinorgbio.2012.02.006
日期:2012.5
2-diamine)platinum(II) complexes connected by a polymethylene chain were synthetized. Activity-structure relationship between amide or ester functionalities was explored by changing acridine-9-carboxamide into acridine-9-carboxylate chromophore. The in vitro cytotoxicity of these new complexes was assessed in human colic HCT 116, SW480 and HT-29 cancer cell lines. Series of complexes bearing the acridine-9-carboxylate
为了改善抗癌药顺铂的药理作用,合成了几种新的通过聚亚甲基链连接的a啶基系链的(乙烷-1,2-二胺)铂(II)配合物。通过将a啶9-羧酰胺转变为a啶9-羧酸盐生色团来探索酰胺或酯官能团之间的活性-结构关系。在体外,这些新的配合物的细胞毒性在人类绞痛HCT 116,SW480和HT-29肿瘤细胞系进行了评估。一系列带有the啶9-羧酸盐生色团的配合物显示出比a啶9-羧酰胺配合物更高的细胞毒性作用,并根据聚亚甲基接头的大小逐渐发挥作用。