Synthesis of 5-N-methyl-benzofuro［3,2-b］quinoline Derivatives and Spectroscopic Studies on These Derivatives as DNA Intercalators

您当前的位置：

首页 >

文章列表页 >

Synthesis of 5-N-methyl-benzofuro［3,2-b］quinoline Derivatives and Spectroscopic Studies on These Derivatives as DNA Intercalators

- Synthesis of 5-N-methyl-benzofuro［3,2-b］quinoline Derivatives and Spectroscopic Studies on These Derivatives as DNA Intercalators
- Vol. 32, Issue 6, Pages: 681-686(2013)
- 作者机构：
  
  1. 广东工业大学轻工化工学院
  2. 广州阳普医疗科技股份有限公司
- 作者简介：
- 基金信息：
- DOI：
  CLC：
扫描看全文
Synthesis of 5-N-methyl-benzofuro［3,2-b］quinoline Derivatives and Spectroscopic Studies on These Derivatives as DNA Intercalators. [J]. 32(6):681-686(2013)
DOI：

Synthesis of 5-N-methyl-benzofuro［3,2-b］quinoline Derivatives and Spectroscopic Studies on These Derivatives as DNA Intercalators. [J]. 32(6):681-686(2013) DOI：

摘要

以生物碱白叶藤碱为出发点，依据生物电子等排体原则，设计了5-N-甲基苯并呋喃［3,2-b］喹啉母体，并参考安吖啶结构特征，合成了一系列5-N-甲基苯并呋喃喹啉的11 位苯胺衍生物，通过波谱手段确认其结构。运用紫外-可见光谱法和分子对接测定了衍生物与DNA的结合常数K和对接分数。紫外光谱实验中，衍生物与小牛胸腺DNA结合后吸收峰出现减色效应和红移现象；离子强度实验排除了表面结合模式的可能性；结合EB置换实验和分子模拟的结果，可初步推断作用模式为嵌插作用。

Abstract

Based on the isostere theory and the structure of alkaloid crytolepine,5-N-methylbenzofuro［3,2-b］quinoline scaffold was designed.Referencing to the derivatization strategy of amsacrine,a series of aniline-substituted 5-N-methylbenzofuro［3,2-b］quinoline derivatives were designed and synthesized,and their structures were characterized by MS and 1H NMR spectra.The binding constants and docking sores of these derivatives with double-stranded DNA were studied by UV-Vis absorption spectra and Surflex-Dock.Surface binding mode was eliminated by ionic strength influence assay.Combined with the results from EB displacement experiments,it was proposed that these derivatives interacted with duplex DNA via intercalation binding mode.

关键词

苯并呋喃［32-b］喹啉双链DNA紫外光谱分子对接EB置换

Keywords

benzofuro［32-b］quinolinedouble-stranded DNAUV-Vis absorption spectramolecular dockingEB displacement

references

Views

1068

下载量

CSCD

Alert me when the article has been cited

提交

Tools

Publicity Resources

Investigation on Interaction between 2,3,3′-Trichloro Biphenyl and Human Serum Albumin by Computer Simulation and Spectroscopy

Study on Flexible Molecular Docking of ACE Inhibitory Tripeptides and ACE

Molecular Mechanism of Inhibition on Tyrosinase Activity by Luteolin

Studies on Interaction between Pentafluoropropioic Acid and Human Serum Albumin by Spectroscopy and Computional Simulations

Study on the Binding Characteristics of 5′-Hydroxy-2,2′,4,4′,5-pentabromo Diphenyl Ether and Human Serum Albumin

Related Author

No data

Related Institution

中国科学院生态环境研究中心

环境化学与生态毒理学国家重点实验室

桂林理工大学化学与生物工程学院

上海海事大学信息工程学院

上海理工大学医疗器械与食品学院

Address：100 Xianlie Middle Road, Guangzhou Postal code：510070
Tel：020-87684776,37656606 Fax：020-87684776 Email：fxcsxb@china.com
Technical support is provided by Beijing Founder electronics co., LTD 粤ICP备12017312号-3 京公网安备11010802024621
It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.

⁰