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Science China Chemistry 2015年第3期58卷 483-494页

作者： Yun-Lei Luo Kishore Baathulaa Vijaya Kumar Kannekanti Cheng-He Zhou Gui-Xin Cai Key Laboratory of Applied Chemistry of Chongqing Municipality Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical Engineering Southwest University Department of Chemistry Kakatiya University Indian Institute of Chemical Technology

A novel series of benzimidazole derived naphthalimide triazoles and some corresponding triazoliums have been successfully synthesized and characterized by 1H NMR, 13 C NMR, 1H-1H COSY, IR and HRMS spectra. All the new compounds were screened for their antimicrobial activities in vitro by two-fold serial dilution. 2-Chlorobenzyl triazolium 8g and compound 9b with octyl group exhibited the best antibacterial activities among all the tested compounds, especially against S. aureus with inhibitory concentration of 2 μg/mL which was equipotent potency to Norfloxacin(MIC=2 μg/mL) and more active than Chloromycin(MIC=7 μg/mL). Triazoliums 8g and 8f bearing 3-fluorobenzyl moiety displayed the best antifungal activities(MIC=2-19 μg/mL) against all the tested fungal strains without being toxic to PC12 cell line within concentration of 128 μg/m L. Further investigations by fluorescence and UV-Vis spectroscopic methods revealed that the compound 8g could effectively intercalate into calf thymus dna to form the 8g-dna complex which could block dna replication, exerting powerful antimicrobial activities.

关键词： naphthalimide benzimidazole triazole antibacterial antifungal calf thymus dna

Design,synthesis,and biological evaluation of novel benzimidazole derivatives and their interaction with calf thymus dna and synergistic effects with clinical drugs

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Science China Chemistry 2014年第6期57卷 807-822页

作者： ZHANG HuiZhen LIN JianMei RASHEED Syed ZHOU ChengHe School of Chemistry and Chemical Engineering Southwest University Sichuan Provincial People's Hospital

A series of new benzimidazole derivatives was synthesized and characterized by IR,1H NMR,13C NMR,MS,and HRMS *** the new compounds were screened for their antimicrobial activities in vitro by a twofold serial dilution *** bioactive evaluation showed that 3,5-bis(trifluoromethyl)phenyl benzimidazoles were comparably or even more strongly antibacterial and antifungal than the reference drugs Chloromycin,Norfloxacin,and *** combination of2,4-difluorobenzyl benzimidazole derivative 5l and its hydrochloride 7 respectively with the antibacterials Chloromycin,Norfloxacin,and the antifungal Fluconazole was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive *** addition,the interaction of compound 5l with calf thymus dna demonstrated that this compound could effectively intercalate into dna to form a compound 5l-dna complex that might block dna replication and thereby exert good antimicrobial activity.

关键词： benzimidazole antibacterial antifungal calf thymus dna synergistic effect

Absorption, Fluorescence and Resonance Rayleigh Scattering Spectra of Interaction of Papain with calf thymus dna

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Chinese Journal of Chemistry 2011年第4期29卷 822-828页

作者：孔玲刘忠芳胡小莉刘绍璞 Luminescence and Real-Time Analysis Key Laboratory of Ministry of Education School of Chemistry and Chemical Engineering Southwest University Chongqing 400715 China

In weak acidic medium, interaction between papain and calf thymus dna （ctdna） resulted in absorption spectral change, fluorescence quenching of papain and remarkable enhancement of resonance Rayleigh scattering （RRS） The interaction types and binding modes were discussed by characteristics of RRS, absorption, fluorescence and circular dichroism spectra combining thermodynamic data. Four interaction types include electrostatic attraction, hydrophobic force, hydrogen bonding and aromatic stacking interaction. Papain interacted with the major groove of ctdna. Aromatic stacking interaction is the main reason of change of absorption spectrum and fluorescence quenching of papain. Surface enhanced scattering effect, resonance energy transfer effect, increase of molecular volume and conformational change make contribution to RRS enhancement. The enhanced RRS intensity （△I） is directly proportional to the concentration of ctdna or papain, The detection limit （3σ） is 5.2 ng·omL^-1 for ctdna and 5.6 ng·mL-1 for papain. This creates conditions for determination of papain and ctdna.

关键词： papain calf thymus dna absorption spectrum fluorescence spectrum resonance Rayleigh scattering

Flow-injection Chemiluminescence Determination of Trace calf thymus dna

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Chinese Chemical Letters 2003年第10期14卷 1051-1053页

作者： Min ZHOU, Yong Jun MA, Xiao Yong JIN, Xiu Lan TENG, Zi Yu ZHANG,Hui CHENInstitute of Chemistry, Northwest Normal University, Lanzhou 730070 Institute of Chemistry Northwest Normal University Lanzhou 730070

A flow injection procedure for the determination of calf thymus DMA （CT dna） over the range 2.1x10-6;.1x10-1 B.g mL-1 is described, based on measurement of the enhanced chemiluminescence emission of rhodamine B-Ce（IV） system, activated by imidazole-HCl buffer solution. This method is highly sensitive, with the linearity range broadened to five orders of magnitude. It has been applied to determine CT dna in synthetic sample with satisfactory results.

关键词： Chemiluminescence flow-injection calf thymus dna imidazole rhodamine B.

Luminescence Studies on Interaction of an Isoquinoline Alkaloid with calf thymus dna in Aqueous Medium and on Solid Substrate

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Chemical Research in Chinese Universities 2012年第4期28卷 614-619页

作者： LI Jun-fenl SHI Wen-tao HAN Xiu-ying DONG Chuan CHOI Martin M.F. School of Chemistry and Chemical Engineering Research Center of Environmental Science and Engineering Shanxi UniversityTaiyuan 030006P.R.China Department of Chemistry Hong Kong Baptist UniversityHong KongP.R.China

The interaction of calf thymus dna（ctdna） with berberine（Ber） was systematically investigated via UV-Vis,fluorescence and phosphorescence spectroscopies in aqueous solution and on solid *** very weak fluorescence intensity of Ber at 525 nm in aqueous solution can be greatly enhanced by *** UV-Vis spectrum shows that Ber could bind with dna by *** addition,strong fluorescence of Ber alone could be observed on filter paper substrate and can be quenched by ctdna effectively,and the increase of fluorescence polarization of Ber on the filter paper implies the intercalation *** emits phosphorescence at 619 nm in the presence of thallium（I） *** lifetime of Ber increased from 38.4 ms to 43.4 ms with the increase of *** increase of lifetime is possibly attributed to the increase of rigidity of Ber after its intercalating into the ctdna base *** explanation is also augmented by the anionic quenching *** behaves as a typical intercalating agent into *** intrinsic binding constant between Ber and ctdna is（1.84±0.12）×10^4 L/mol and n=0.16.

关键词： Berberine calf thymus dna UV-Vis spectroscopy Luminescence Interaction

Ruthenium Coordination Compounds with Polypyridines(Ⅵ)--Interaction of Ruthenium Polypyridine Complexes with calf thymus dna-An Example of Non-intercalative Binding

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Chemical Research in Chinese Universities 1997年第4期13卷 3-8页

作者： YANG Guang WANG Lei WU Jian-zhong ZENG Tian-xian JI Liang-nian Department of Chemistry Zhongshan UniversityGuangzhou510275 State Key Laboratory for Oxa Synthesis and Selective Oxidation Lanzhou Institution of Chemical PhysicsChinese Academy of SciencesLanzhou730000

Two new ruthenium polypyridine complexes, L 2RuL 2+ (L represents 2,2 bipyridine(bpy) or 1,10 phenanthroline(phen); L  represents Schiff base derived from 4,5 diazafluoren 9 one(AFO) and n propylamine) have been prepared and characterized by means of elementary analyses, electronic absorption and IR spectra. The binding of the complexes to calf thymus dna has been investigated via absorption, emission spectrometry, emission quenching, equilibrium dialysis and circular dichroism spectrometry. The experimental results show that these two complexes bind to calf thymus dna by electrostatic mode and by non intercalative binding mode respectively.

关键词： Ruthenium Polypyridine calf thymus dna

Synthesis,Crystal Structure and Interaction with calf thymus dna of Transition Metal Complex with 2'-(4-Dimethylaminobenzylidene)-2-hydroxybenzoylhydrazide

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Synthesis,Crystal Structure and Interaction with Calf Thymus...

Study of two camptothecins binding to calf thymus dna by spectroscopic techniques and molecular docking

2010中西部地区无机化学化工学术研讨会

作者： WANG Liu-Jie~1,GUO Hui-Lin~1,CHEN Feng-Ying~2,HE Shui-Yang~(1*) (1 College of Chemistry & Materials Science,Northwest University,Key Laboratory of Synthetic and Natural Functional Molecule Chemistry(Ministry of Education),Shaanxi Key Laboratory of Physico-Inorganic Chemistry,Xi’an,710069,China 2 Department of Chemistry and chemical engineering, Shangluo University,Shangluo 726000,China)

A series of single-ligand transition metal complexes of the general formula M(HL)(where HL=2’-(4-dimethylaminobenzylidene)-2-hydroxybenzoylhydrazide,M=Ni,Cu,Zn,Cd.) were prepared and characterized with elemental analyses,spectroscopic(IR,UV-vis) and the crystal structure of Ni(HL) was characterized by a single crystal X-ray *** coordination environment around the Ni ion might be described as a distorted *** interaction of these complexes with calf thymus dna(CT-dna) was studied and investigated by electronic absorption titration(UV spectroscopy) and fluorescence emission titration(fluorescence emission spectra,quenching spectra and emission spectra of interaction with ethidium bromide(EB)-dna system).The results show that these complexes are bound to CT-dna mainly by intercalation *** present paper,Ni(HL) was selected as a representative sample.

关键词： Crystal Structure calf thymus dna Intercalation

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Study of two camptothecins binding to calf thymus DNA by spe...

Studies on the Interaction of Cobalt Mixed-Ligand Coordination Compound Containing Tetrapyrido [3,2-a:2′,3′-c:3″, 2″-h:2■,3■-j] phenazine with dna

中国化学会第七届全国热分析动力学与热动力学学术会议

作者： Sheng-Chao Huang Yi Wang Meng-Yuan Ji Yan-Jun Hu Hubei Key Laboratory of Pollutant Analysis ＆ Reuse Technology Department of ChemistryHubei Normal University

Camptothecin is a hydrophobic plant alkaloid isolated from Camptotheca acuminate,which has been demonstrated to be an effective agent works against a broad spectrum of human cancers,such as colon,lung,breast,ovarian and so on;ascribe its binding to topoisomerase I to inhibit dna replication and RNA transcription processes,this has aroused great interest in the scientific and medical *** acid（dna） is the important genetic material of living organisms,and also the target of many *** interaction between drug molecules and dna has attracted extensive attention in recent years,because the interaction between the two is not only helpful to reveal the mechanism of action of drugs,but also has important significance for the research and development of new *** this study,camptothecin（CPT） and hydroxycamptothecin（H-CPT） has been employed to binding with calf thymus dna（ctdna）,by using multi-spectroscopic methods and molecular docking study.

关键词： Camptothecin calf thymus dna multi-spectral molecular docking

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Chemical Research in Chinese Universities 2001年第3期17卷 243-248页

作者： SONG Yu-fei YANG Pin Institute of Molecular Science Shanxi UniversityTaiyuan 030006P.R.China

A new monometallic complex [Co(phen)_2tpphz]^(3+) (where tpphz is tetrapyrido [3,2-a:2′,3′-c:3″,2″-h:2′″,3′″-j] phenazine) was synthesized by the reaction of 5, 6-diamino-1,10-phenanthroline with [Co(phen)_2(phendione)]^(3+). It was characterized by elemental analysis, molar conductivity, IR, ~1H NMR, ultraviolet and fluorescence spectroscopy. The interaction of the complex with dna was also investigated. The complex shows the absorption hypochromicity, fluorescence enhancement, the specific viscosity increased when bound to calf thymus dna. The cyclic voltammetry (CV) measurement showed a change in peak current with the addition of dna. All the results provide the support for the intercalative binding mode of the mononuclear complex.

关键词： Tetrapyrido [3,2-a: 2′,3′-c: 3″,2″h, 2~■,3~■-j] phenazine Cobalt calf thymus dna Intercalative Binding mode

Coumarin-derived azolyl ethanols:synthesis,antimicrobial evaluation and preliminary action mechanism

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Science China Chemistry 2016年第7期59卷 878-894页

作者： Xin-Mei Peng Kannekanti Vijaya Kumar Guri L.V. Damu Cheng-He Zhou Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China

A series of coumarin-derived azolyl ethanols including imidazolyl,triazolyl,tetrazolyl,benzotriazolyl,thiol-imidazolyl and thiol-triazolyl ones were conveniently synthesized and characterized by IR,~1H NMR,^(13)C NMR and high-resolution mass spectra(HRMS) *** of the prepared compounds showed appropriate logP_(ow) values and effective antibacterial and antifungal ***,compound 14 with bis-triazolyl ethanol group exhibited low minimal inhibitory concentration(MIC)value of 8 μg/mL against MRSA,which was comparable or even superior to reference drugs Norfloxacin(MIC=8μg/mL)and Chloramphenicol(MIC=16μg/mL).It could also effectively inhibit the growth of the tested fungal strains compared to *** binding studies of coumarin 14 with calf thymus dna were investigated by UV-Vis absorption and fluorescence *** was found that compound 14 could interact with calf thymus dna by groove binding to form14-dna complex via both hydrogen bonds and van der Waals force,which might be the factor to exert the powerful antimicrobial activity.

关键词： coumarin imidazole triazole tetrazole antibacterial antifungal calf thymus dna