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Novel N-(3-carboxyl-9-benzylcarboline-1-yl) ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA
Wu, Jianhui; Cui, Guohui; Zhao, Ming; Cui, Chunying; Peng, Shiqi
刊名MOLECULAR BIOSYSTEMS
2007
DOI10.1039/b712092n
3期:12页:855-861
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemistry & Molecular Biology
研究领域[WOS]Biochemistry & Molecular Biology
关键词[WOS]BOVINE SERUM-ALBUMIN ; BETA-CARBOLINE ; ANTINEOPLASTIC AGENTS ; BIOLOGICAL-ACTIVITY ; CYTOTOXIC ACTIVITY ; CRYSTAL-STRUCTURE ; ANTITUMOR AGENTS ; IN-VITRO ; BINDING ; DERIVATIVES
英文摘要

To explore the intercalating mechanism of beta-carbolines, four novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids [-phenylalanine (6a), -alanine (6b), -isoleucine (6c) and -glycine (6d)] were prepared here. Their in vitro anticancer activities were examined by their anti-proliferation for 5 human carcinoma cell lines. The average IC(50)s against 5 human carcinoma cell lines are 53.54 mu M, 118.77 mu M, 147.34 mu M and greater than 291.63 mu M for 6a, 6b, 6c and 6d, respectively. The DNA intercalating mechanism of 6a-d was approved by the comparison of the parameters and signals of UV, CD and fluorescence spectra of calf thymus DNA (CT DNA) alone and the CT DNA/6a-d system. Using fluorescence titration based kinetic analysis a two-step-course consisting of stacking and intercalating was described and the stacking was considered as the key step to the CT DNA intercalating mechanism of 6a-d. Using fluorescence titration based thermomechanical analysis, the stacking complexes of 6a-d with CT DNA were described to be formed spontaneously and to be stabilized predominantly by their hydrophobic interactions. The intercalation itself goes very fast and only has limited contribution to their anticancer activities.

语种英语
WOS记录号WOS:000250932100014
引用统计
被引频次:18[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/67390
专题北京大学药学院
作者单位1.Peking Univ, Coll Pharmaceut Sci, Beijing 100083, Peoples R China
2.Capital Med Univ, Coll Pharmaceut Sci, Beijing 100069, Peoples R China
推荐引用方式
GB/T 7714
Wu, Jianhui,Cui, Guohui,Zhao, Ming,et al. Novel N-(3-carboxyl-9-benzylcarboline-1-yl) ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA[J]. MOLECULAR BIOSYSTEMS,2007,3(12):855-861.
APA Wu, Jianhui,Cui, Guohui,Zhao, Ming,Cui, Chunying,&Peng, Shiqi.(2007).Novel N-(3-carboxyl-9-benzylcarboline-1-yl) ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA.MOLECULAR BIOSYSTEMS,3(12),855-861.
MLA Wu, Jianhui,et al."Novel N-(3-carboxyl-9-benzylcarboline-1-yl) ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA".MOLECULAR BIOSYSTEMS 3.12(2007):855-861.
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