Determination of binding modes and binding constants for the complexes of 6H-pyrido[4,3-b]carbazole derivatives with DNA

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• 作者：Akihito Shimazu^a ; Masashi Kawagoshi^a ; Shoichi Takeda^a ; Haruaki Kurasaki^a ; Asako Kato^a ; Nahoko Morii^b ; Norio Sakai^a ; Takeo Konakahara^a ; ^{konaka@rs.noda.tus.ac.jp}
• 关键词：Ellipticine ; 6H-Pyrido[4 ; 3-b]carbazole ; DNA ; Intercalation ; Binding constant ; QCM ; Deflection spectroscopy ; Molecular modeling ; GC base-pair preference ; Salt effects ; pH dependence ; Cytotoxic activity
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 February 2017
• 年：2017
• 卷：25
• 期：3
• 页码：1094-1112
• 全文大小：1889 K
• 卷排序：25

文摘

The binding modes for DNA-complexes of 40 pyridocarbazoles were determined. The binding constants Ka for DNA-complexes of 40 pyridocarbazoles were determined. Some of these compounds exhibited potent GC-pair preference. Ka’s of 2-(ω-amino)alkyl compounds were larger than those of 5-(ω-amino)alkylcarbamyl. Framework of 2-tethered compound completely overlapped with stacking DNA-GC base-pairs.