Choudhury Jayati Roy, Guddneppanavar Rajsekhar, Saluta Gilda, Kucera Gregory L, Bierbach Ulrich
Department of Chemistry, Wake Forest University, Winston-Salem, NC 27109, USA.
J Med Chem. 2008 Jun 12;51(11):3069-72. doi: 10.1021/jm8003569. Epub 2008 May 6.
Four highly charged, water soluble platinum-acridine bisintercalating agents have been synthesized. Depending on the cis/trans isomerism of the metal and the nature of the acridine side chains, bisintercalation induces/stabilizes the classical Watson-Crick B-form or a non-B-form. Circular dichroism spectra and chemical footprinting experiments suggest that 4, the most active derivative in HL-60 cells, produces a structurally severely perturbed DNA with features of a Hoogsteen base-paired biopolymer.
已合成了四种高电荷、水溶性的铂-吖啶双插入剂。根据金属的顺式/反式异构现象以及吖啶侧链的性质,双插入会诱导/稳定经典的沃森-克里克B型或非B型。圆二色光谱和化学足迹实验表明,4(HL-60细胞中最具活性的衍生物)产生一种结构上严重扰动的DNA,具有Hoogsteen碱基配对生物聚合物的特征。