alexa Synthesis, DNA-binding Properties and Quantitative Structure-Activity Relationships on Ruthenium(II) Complexes with Calf-Thymus DNA
ISSN: 2161-0444

Medicinal Chemistry
Open Access

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Research Article

Synthesis, DNA-binding Properties and Quantitative Structure-Activity Relationships on Ruthenium(II) Complexes with Calf-Thymus DNA

Hao Zhang1, Fan Yang1, Qiong Wu2, Si-Yan Liao3, Ping Liu4, Wen-Jie Mei2*, Li Li3, Shuang-Yan Zhang3 and Xi-Cheng Wang1*

1The First Affiliated Hospital of Guangdong Pharmaceutical University, Guangzhou, 510006, PR China

2The Pharmacy Department of Guangdong Pharmaceutical University, Guangzhou, 510224, PR China

3School of Pharmacy, Guangzhou Medicine University, Guangzhou 510275, PR China

4The Chemistry Department of Hu’nan Arts and Philosophy Science University, Changde, 415000, PR China

*Corresponding Author:
Xi-Cheng Wang
The First Affiliated Hospital of Guangdong
Pharmaceutical University
Guangzhou, 510006, PR China
Tel: 86- 20-61321397
E-mail: [email protected]
Wen-Jie Mei
The Pharmacy Department of Guangdong
Pharmaceutical University
Guangzhou, 510224, PR China
Tel: 86-20-39352129
E-mail: [email protected]

Received date: February 25, 2016; Accepted date: March 08, 2016; Published date: March 10, 2016

Citation: Zhang H, Yang F, Wu Q, Si-Yan L, Liu P, et al. (2016) Synthesis, DNA-binding Properties and Quantitative Structure-Activity Relationships on Ruthenium(II) Complexes with Calf-Thymus DNA. Med chem (Los Angeles) 6:137-142. doi:10.4172/2161-0444.1000338

Copyright: © 2016 Zhang H, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.



A series of novel ruthenium(II) complexes with electron-donor or electron-acceptor groups in intercalative ligands, [Ru(phen)2(o-MOPIP)]2+(1), [Ru(phen)2(o-MPIP)]2+(2), [Ru(phen)2(o-CPIP)]2+(3) and [Ru(phen)2(o-NPIP)]2+(4) have been synthesized and characterized with elementary, ES-MS, 1H NMR, electronic absorption and emission spectra. The binding properties of these complexes to CT-DNA have been investigated by spectroscopy and viscosity experiments. It’s illustrated that these complexes bind to DNA in a non-classical intercalation mode and their intrinsic binding constants (Kb) for 1, 2, 3 and 4 are calculated as 1.1, 0.35, 0.53 and 1.7 × 105 M-1, respectively. The Quantitative Structure-Activity Relationships (QSAR) of these ruthenium complexes, as well as some other ruthenium complexes congers has been investigated, and a linearity equation have been obtained: logKb=0.2429π+0.0429π2+0.2907σ+0.6 389I+4.3491 (n=12; R=0.9338; F=11.9134; p=0.0030). This results show that the electron-acceptor group and a large hydrophobic group will enhance the DNA binding affinity of ruthenium complexes.


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