Tuning the DNA Conformational Perturbations Induced by Cytotoxic Platinum−Acridine Bisintercalators: Effect of Metal Cis/Trans Isomerism and DNA Threading Groups

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• 作者：Jayati Roy Choudhury ; Rajsekhar Guddneppanavar ; Gilda Saluta ; Gregory L. Kucera ; Ulrich Bierbach
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：June 12, 2008
• 年：2008
• 卷：51
• 期：11
• 页码：3069 - 3072
• 全文大小：451K
• 年卷期：v.51,no.11(June 12, 2008)
• ISSN：1520-4804

文摘

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.