2,5-dimethylpiperazine is an important chemical material and pharmaceutical intermediate. It could be used in the synthesis of a number of fine chemicals including Pharmaceuticals, pesticides, dyestuffs, surfactants, etc. 2,5-dimethylpiperazine could be obtained by reduction of 3,6-dimethyl-2,5-diketopiperazine、2,5-dimethylpyrazine or catalytic hydrogenation of lactamide or isopropanolamine. In this thesis, isopropanolamine was used as reactant to form 2,5-dimethylpiperazine in the presence of hydrogenation-dehydrogenation catalysts, e.g. Raney-Ni. The reaction conditions were optimized, such as the amount of the catalyst、reaction temperature、reaction pressure and reaction time. The optimum processing conditions: 2.0～3.0 MPa original hydrogen、reaction temperature 150～170℃, 2.5～5.0 grams of Raney-Ni catalyst per mole and a reaction time of 4 to 6 hours. Under these conditions, the conversion of isopropanolamine was 100 % and the yield of 2,5-dimethylpiperazine was about 70%. The reaction conditions were much moderate compared to references, e.g. the reaction pressure drop from 8.0 MPa to 4.0 MPa and the reaction temperature drop about 50℃. Reaction with Ni-B amorphous alloy catalysts、Ni-B amorphous alloy catalysts with addition of Mo and Cu/SiO2 were also studied. But all of the yields and coversion were much lower. 2,5-dimethylpiperazine, which purity was 90%, was obtained by rectification. And 2,5-dimethylpiperazine of 99 % purity was got by recrystallization. The result ratio of 2,5-dimethylpiperazine against 2,5-dimethylpyrazine could be regulated according to reaction temperature, initial pressure, etc. For example, 2,5-dimethylpyrazine could be obtained by a high yield of 74.5% when reacting at 240℃for 6 h with 1.25 g·mol-1 Raney Ni catalyst and zero initial pressure.
Post about "2"
The main purpose of this paper is to modify supported Ziegler-Natta catalysts through their reaction with some specific organic compounds,in order to alter the nature and distribution of the active sites（C*）,thereby control the chemical composition distribution（CCD）of ethylene-α-olefin copolymers（or:linear low density polyethylene,LLDPE）.Firstly,an industrial supported Ziegler-Natta catalyst（cat-1）is modified by treating it with 2,6 – diisopropyl phenol,getting the modified catalyst cat-2.The two catalysts were used for ethylene and 1-hexene copolymerization in different comonomer concentration.The copolymers were characterized by 13C-NMR and GPC.Experimental study found,comonomer effect of cat-2 is weaker than cat-1. In copolymerization with cat-2,the activity reached the maximum value at relatively low 1-hexene concentration.With increasing comonomer concentration, the molecular weight of copolymer catalyzed by cat-2 declines much slower than cat-1.13C-NMR analysis showed that the copolymer catalyzed by cat-2 is more uniform in comonomer distribution than copolymer catalyzed by cat-1,especially the catalytic system activated by MAO.Secondly,a supported Ziegler-Natta catalyst TiCl4/MgCl2（cat-3）was prepared, then it was modified by 2,6 – diisopropyl phenol,getting the modified catalyst cat-4.The two catalysts were used for ethylene and 1-hexene copolymerization and copolymerization in the presence of a small amount of hydrogen.The copolymers were characterized by 13C-NMR and GPC.The experiment results showed that, comonomer effect of cat-4 is weaker than cat-3,as revealed by 13C-NMR analysis of the copolymer’s soluble and insoluble fractions in boiling n-heptane,the 1-hexene content in the two fractions is much closer in copolymer catalyzed by cat-4 than cat-3,so the copolymer by cat-4 has more uniform comonomer distribution,especially the catalytic system activated by MAO.The decline of activity with hydrogen amount in the polymerization with cat-4 is slower than with cat-3.In the presence of hydrogen,the copolymer catalyzed by cat-4 also showed a more uniform comonomer distribution than cat-3,especially when the catalytic system was activated by MAO.In general,these changes are beneficial to the synthesis of ethylene-α-olefin copolymers with narrower distribution of composition.1-Hexene homopolymerization catalyzed by cat-3 and cat-4 were also studied. The number of the active（Cp）center in the catalytic systems was determined using a method based on quenching reaction by cinnamoyl chloride.The average polymerization activity of active sites of cat-4 is less than cat-3,maybe some active site in cat-3 catalyst is deactivated by 2,6 – Diisopropyl phenol.When adding a small amount of hydrogen to 1-hexene homopolymerization system,Cp of all the catalytic systems decreased,in which cat-4 reduced more significantly.Based on the main results of this work,the mechanism of catalyst modification by phenoxy ligand was discussed,and two possible models of the interaction between the phenoxy ligand and the active centers were proposed.
The present thesis relates to the synthesis of 2′-O-benzoyl-5′-O-（4,4′-dimethoxytrityl） N4-acetyl-2′,3′-secocytidine and 2′-O-benzoyl-5′-O-（4,4′-dimethoxytrityl）-N2-isobutyryl-2′,3′-secoguanosine. They are an important intermediate for the preparation of oligonucleotide. So the research on synthesis of the nucleoside derivatives was of great practical significanc. The final products were identified by IR and 1H NMR.The synthesis of 2′-O-benzoyl-5′-O-（4,4′-dimethoxytrityl）-N4-acetyl-2′,3′-secocytidine comprises the following steps: DMT-Cl（4,4′-dimethoxytritylchloride） reacted with N4-acetylcytidine in prydine is converted to 5′-O-（4,4′-dimethoxytrityl）-N4-acetylcytidine, which is oxidated by NaIO4 and reductived by NaBH4 to give5′-O-（4,4′-dimethoxytrityl）-N4-acetyl-2′,3′-secocytidine. Acylatel with benzonychloride affords final product in the total yield 41%.Preparation of the 2′-O-benzoyl-5′-O-（4,4′-dimethoxytrityl）-N2-isobutyryl-2′,3′-secoguanosine starts from guanosine. Guanosine is acylated by isobutyryl chloride provide N2-isobutyrylguanosine. DMT-Cl reacted with N2-isobutyrylguanosine in prydine is converted to 5′-O-（4,4′-dimethoxytrityl）-N2-isobutyrylguanosine, which is oxidated by NaIO4 and reductived by NaBH4 to give 5′-O-（4,4′-dimethoxytrityl）-N2-isobutyryl-2′,3′-secoguanosine. Acylatel with benzony chloride affords the key intermediate is formed in 28% yield.
Syntheses, Characterization, Structure and Properties of Complexes with Terpyridine and Terpyridine-like Ligands
One of the most important used in modern coordination chemistry is the aspect of N-heteroaromatic ligands, which largely based on pyridine, 2,2′-bipyridine, melamine, and 2,2′:6′,2″-terpyridine （simply terpyridine）, have become an ever-expanding synthetic, application and structural frontier. Terpyridine ligands and the tailored terpyridine derivatives （especially 4′- functionalized terpyridines） are stronge tridentate ligands and have much advances and ever-expanding potential applications. Their well-known characteristics are applied in the fields of optical, catalytic, molecular recognition, gas storage, solar cell and so on. Also they could self-assemble lots of intriguing topological structures.Firstly, this thesis focuses on the synthesis of three 4′- functionalized terpyridine with 4-hydroxyphenyl、2-furyl and carboxylic acid. Several coordination compounds have been prepared by the reaction of d10 metals (Cd2+、Zn2+) with these ligands. All compounds are characterized by elemental analysis, IR, emission spectra and single-crystal X-ray diffraction.On the other hand, we think melamine and 2,6-bis（2-furyl）pyridine are very useful terpyridine-like ligands. Three novel melamine complexes with copper（II） including sandwich and extensive hydrogen bonds were obtained. Moreover, a new ligand of 4-（4′-Hydroxyphenyl）-2,6-bis（2-furyl）pyridine has been synthesized and may be uesd as pH sensor.In detail, the work is divided into six chapters as following:In Chapter 1, the research background of the synthesis of 4′-functionallized terpyridine and the current survey of terpyridine coordination compounds in particular optical properties and supermolecular assemblies are concisely introduced. A survey of melamine and 2,6-bis（2-furyl）pyridine are also mentioned.In Chapter 2, the cadmium（II） complex, Cd（p-HO-ptpy）Cl2, p-HO-ptpy being a tridentate ligand 4′-（4-hydroxyphenyl）-2,2′:6′,2″-terpyridine has been synthesized and the crystal structure is determined using X-ray crystallography. Furthermore, its luminescent and electrochemical properties compared with the ligand have been investigated.In Chapter 3, the cadmium（II） complex, [Cd（ftpy）I2]·CHCl3, which ftpy being a ligand of 4′-（2-furyl）-2,2′:6′,2″-terpyridine has been synthesized. Furthermore, its crystal structure and luminescent properties compared with the ligand have been investigated.In Chapter 4, five mononuclear complexes c1-c5 and a mononuclear polymer c6 containing the ligand of 2,2′:6′,2″-terpyridine-4′-carboxylic acid （Hctpy） were prepared by hydrothermal method. The metallic ions in c1-c5 have distorted octahedral coordinations with six nitrogens from two molecules of Hctpy. But 1D chain structure of complex c6 is built by carboxylic acid of Hctpy and resulted in the enhanced emission band. The coordination mode of c6 has never been reported.In Chapter 5, a new ligand of 4-（4-Hydroxyphenyl）-2,6-bis（2-furyl）pyridine had been synthesized by two methods. Furthermore, this compound exhibits novel ultraviolet and electrochemical properties under the influence of pH value. The reason and the mechanism of Hpfpy may be tentatively assigned.In Chapter 6, three copper（II） coordination compounds have been synthesized and researched by cyclic voltammograms. Two novel melamine coordination compounds of them including the copper directly bonded to the aromatic rings of melamine have extensive hydrogen bonds and consolidate a 2-D sheets. Interestingly, one is a dinucear complex with a paddle wheel structure in which the apical positions are occupied specially by two different donor ligands.
Phenols are important chemicals and widely existed in various natural products.Their 2,6-di-substituted derivatives are useful intermediates for constructing highly functionalized biologically and medicinally important products.Hindered phenols are a kind of important antioxidants,they are widely used on the antioxidants of plastic.Their other derivatives have been intensely investigated in view of their applications as antibiotics and antitumor agents. Very often,their preparation requires a multistep raction,involves a expensive oxidant,or pollute the environment.This thesis first time takes the nitrous oxide as oxidant,the methanol as solvent,carrying on seleetivity oxidation study on 2,6-di-tert-butyl-4-methylphenol and 2,4,6-trimethylphenol. Their structures were characterized by melting point,LC-MS and ~1H NMR method.The effects of reaction time,reaction temperature and the amount of nitrous oxide on conversion and selectivity were investigated and we found out the optimal condition:temperature 40℃, time 8 hours.The conversion of 2,6-di-tert-butyl-4-methylphenol is 63%,and the selectivity of 2,6-di-tert-butyl-4-methoxymethylphenol is 88%;the conversion of 2,4,6-trimethylphenol is 81%,and the selectivity of 2,6-dimethyl-4-methoxymethylphenol is up to 99%.The other substituted phenols were also studied tentatively.The other solution of alcohol was compared,and we got the corresponding ethers.Their structures were also characterized by melting point,LC-MS and ~1H NMR method.The yield of product is lower as the polarity of O-H weaker.Reaction mechanism was discussed.The conditions of acid and alkali were investigated and we got 4-hydroxy-2,4,6-trimethyl-cyclohexa-2,5-dienone in alkali condition.
Flupirtine, is a new kind of moderate intensity of the central non-opioid analgesics, small adverse reaction, non-addictive, effective to many kinds of aches. Besides, it can be used in many indications (such as anticonvulsant, cell protection, treatment of movement disorders and rigid caused by lacking of dopamine, anti-Parkinsonian, anti-migraine, anti-inflammatory, and so on), showing a broad clinical application prospect. But it has not been registered in China, and the synthesis of flupirtine and 2,3,6-triaminopyridine derivatives has not been reported in domestic yet. Therefore, the synthesis and process optimization of Flupirtine is very significance.In this paper, A five-step procedure and optimization for synthesis of flupirtine maleate, started from 2,6-dichloro-3-nitropyridine, was developed. Ethanol replaced dioxane as solvent, the total yield of the five-step up to 81.2%. In addition, seven 2,3,6-triaminopyridine derivatives were deigned and prepared, four of them has not been reported in the literature. The test of antioxidant activity by the elimination of DPPH radical showed that the six of 2,3,6-triaminopyridine derivatives have antioxidation activity.Moreover, flupirtine maleate reference substance was prepared, and HPLC methods were empoldered and tested:λ=248 nm, pH=3.65, methanol-water (55-45); the range of concentration is 0.01-0.90 mg/ml, linear regression equation for Y = 1488842X + 89008, R~2=0.9999; the average recovery was 100. 6% (RSD=0.77%, n=9).A new route of nevirapine was studied. Found that the the selectivity of acylation between 2,3-diamino-4- methyl-pyridine and 2-chloronicotinoyl chloride was not existed, and the product ring-closured easily.
Sulfur dioxide（SO2） is an important air pollutant all over the world, which exists as low concentrations in the atmosphere and high concentrations in some industrial areas.High doses of SO2 exposure make city environment deteriorated and have severely threatened human health.Many studies of epidemiology show that SO2 can not only cause respiratory tract diseases,but also affect cardiovascular system and genital system.Toxicology evidences also indicate that SO2 may cause toxicological damage to multiple organs of animals,and some of them are even severer than damages in lungs.Recently few data are available on the effects of exposed to the pollutant on the molecular mechanism,although some biochemical changes,genetic toxicity, oxidative stress and DNA damage have been detected.In order to explore the role of SO2 on protein oxidative damage in mice and its molecular mechanism,the effects of protein and DNA damage of SO2 in different organs and tissues were studied.It will provide based data for the protein oxidative damage,nucleic acid damage,the occurrence of diseases, development,the prevention,control and clinical diagnosis.The mice were treated with SO2 at different concentrations（0,14,28 and 56 mg/m3） for 6 hours per day for 7 days.The protein carbonyl（PCO） content was measured by using spectrophotometric DNPH assay,and the DNA-protein crosslinks （DPC） coefficient was measured by using KCl-SDS assay.It will be used to estimate the degree of oxidative damage of protein and nucleic acid induced by SO2.1.Effects of sulfur dioxide on protein carbonyl（PCO） content in different tissues of mice When the concentration of SO2 was 14 mg/m3,it could induce the increase of PCO levels in hearts,livers,lungs,brains,spleens,kidneys and stomachs of female and male mice.Compared with the control,PCO contents in livers and lungs of female mice have highly significant and very significant increase（P＜0.01 and P＜0.001）,while PCO contents in livers, lungs and spleens of male mice have very significant increase（P＜0.001）, PCO contents in kidneys and stomachs have significant increase（P＜0.05）. When the concentrations of SO2 were 28 mg/m3 and 56 mg/m3,PCO contents in seven tissues of female and male mice have significant increase（female: stomach P＜0.05,heart,brain and spleen P＜0.01,liver,lung and kidney P＜0.001 male:stomach P＜0.05,brain and kidney P＜0.01,heart,liver,lung and spleen P＜0.001）.As the concentration of SO2 increases,PCO contents continue to increase（female:stomach P＜0.05,heart,liver,lung,brain,spleen and kidney P＜0.001 male:kidney and stomach P＜0.01,heart,liver,lung, brain and spleen P＜0.001）.Through the comparison of male and female mice, it could be concluded that the PCO levels of heart and liver have differences between female and male mice at the concentration of 56 mg/m3（P＜0.05）.It showed that protein oxidative damage to the female mice is more serious.2.Effects of sulfur dioxide on DNA-protein crosslinks（DPC） content in different histiocytes of miceWhen the concentration of SO2 was 14 mg/m3,it could induce the increase of DPC%levels in hearts,livers,lungs,brains,spleens,kidneys and stomachs of female and male mice.Compared with the control,DPC% contents in lungs and kidneys of female mice have significant and highly significant increase（P＜0.05 and P＜0.01）,while DPC%contents in spleens and kidneys of male mice have significant increase（P＜0.05）.When the concentrations of SO2 were 28 mg/m3 and 56 mg/m3,DPC%contents in seven histiocytes of female and male mice have significant increase（female: brain and stomach P＜0.05,kidney P＜0.01,lung and spleen P＜0.001 male: heart,liver and stomach P＜0.05,lung and spleen P＜0.01,kidney P＜0.001）. As the concentration of SO2 increases,DPC%contents continue to increase （female:brain P＜0.05,heart,liver,lung,spleen and kidney P＜0.001 male: stomach P＜0.05,heart,liver,lung,spleen and kidney P＜0.001）.Through the comparison of male and female mice,it ccould be concluded that DPC% contents of lungs,brains and stomachs have differences between female and male mice at the concentration of 56 mg/m3（P＜0.05）.The damage to the female mice is more serious.When the concentrations of SO2 were 28 and 56 mg/m3,DPC%levels had also differences in spleens（P＜0.01）.But DPC% contents in the other histiocytes had no differences between female and male mice.3.ConclusionIn all,SO2 exposure could cause the formation of PCO and DNA-protein crosslinks（DPC） in hearts,livers,spleens,lungs and kidneys of mice compared with the control at the concentration of 14 – 56 mg/m3.The increases of PCO and DPC contents share the same regulation in a concentration（SO2）-dependent manner.The concentration-response linear equations and the related correlation coefficients are higher than 0.9.Its toxicological mechanism may be that when SO2 was inhaled into the body,it could induce the body to produce.OH and O2-.or inhibite the activity of the body antioxidase.At last it would cause the accumulation of excessive free radical,even damaged protein and DNA of the body.Through the comparison of male and female mice,it can be concluded that the PCO levels of hearts and livers and the DPC%levels of lungs,brains and stomachs have differences between female and male mice at the concentration of 56 mg/m3 （P＜0.05）;when the concentrations of SO2 were 28 and 56 mg/m3,DPC% levels have also differences in spleen（P＜0.01）.Generally speaking,protein oxidative damage and DPC%levels to the female mice are more serious.The results support the topic that SO2 is a systemic toxicant.
Chitosan is a production of the chitin part takes off acetyl-group, chitin is the second amyloses only next to cellulose broad exist in low grade animals such as crab, shrimp and in low grade plants such as alga, fungus. Its contents are extremely rich, nature output every year may amount to 10 tons . It has recently attracted great attention of numerous investigators in different countries because of its unique chemical and biological properties.The first part of this paper dealt with the factors affecting the preparation of 2-Hydroxypropyltrimethyl ammonium chloride chitosan (CTS-ETA). In order to obtain the optimum process conditions, the effects of some factors, such as dosage of etherifying agent, reaction time, reaction temperature or reaction ratio, degree of substitution ,were studied. The chitosan quaternary ammonium salt was characterized by fourier transform infrared spectroscopy (FTIR)Secondly, a copolymer was obtained from graft copolymerization of 2-Hydroxypropyltrimethyl ammonium Chloride Chitosan and acrylamide in nitrogen atmosphere by using ceric ammonium nitrate as redox initiator. It was found that the grafting percentage is 29.5%, viscosity is highter than 57mpas when the concentration of reaction temperature is 35℃, reaction time is 4h. The grafted copolymer was identified by FT-IR.In the third part, the effect of CTS-ETA on the physical properties, aging resistance properties and antibacterial activity of handsheets were studied in this part, the product with different DS and concentration was sprayed on the handsheets or internal added in the pulp respectively. The result showed that the properties of handsheets internal added by DS 1.015 and concentration of 0.2% CTS-ETA changed greatly, the tensile strength increased 15.7 %, the folding endurance increased nearly 54%, and the tearing index and bursting index increased 12.8% and 16.6% respectively. When the handsheets were treated by sprayed the tensile strength, folding endurance, the tearing index and bursting index increased 18.5%,29.7%,15.5%,18.8% respectively. Aging resistance could also be improved by treatment of CTS-ETA, but there is no influence on brightness and gloss.The effect of CTS-ETA on the antibacterial activity of handsheets was investigated. It was showed that the obtained quaternary ammonium salt of chitosan was water soluble and was of good antibacterial effect with low dosage. The handsheets which treated by internal added in the pulp with CTS-ETA (DS=1.015) at a concentration of 0.25% inhibit the growth of Gram negative bacteria ( Escherichia coli) and Gram positive bacteria ( S taphylococcus aureus).The inhibitory ratio to each of them is 63.5%,73.2%. The handsheets which treated by sprayed on the handsheets could inhibit the growth of S. aureus completely at a solution concentration of 0.25% (DS=1.015) and could inhibit 90% of E.coli’s growth. The CTS-ETA definitely has an inhibitory activity against S. aureusa and E. coli.The CTS-ETA-g-AM can be used as paper strengthen agents. The experiments showed that they can improve the physical properties of handsheets made of softwood pulp. adding only 0.3% dosage of the derivates in the pulp the tensile strength, tearing index, bursting index and folding endurance increased 18.1%, 6.9%, 17.1% and 56%, respectively, CTS-ETA-g-AM (viscosity=57mpas) could inhibit the growth of E.coli and S.aureus significantly. The inhibitory ratio reached 29.4% and 57.8% for E. coli and S.aureus at a concentration of 0.3%.
A mutation strain Klebsiella sp. UN-79 was obtained with stable genetic character, after being treated with UV、NTG and the fast screening method based on acid production and 2,3-butanediol tolerance. Then the fermentation medium and fermentation conditions were optimized. The main research contents and results are follows:1. The combined mutation of UV and NTG on Klebsiella sp was conducted, and the fast screening method based on acid production and 2,3-butanediol tolerance were established. After that, the 2,3-butanediol production ability was increased to 24.20 g/L, which was 3.8 times than that of the wild type. Moreover, heritage stability was confirmedafter several generations of subclonation and physiological and biochemical tests.2. Effect of carbon source, nitrogen source, mineral salt and metal ion on the cell growth and 2,3-butanediol production of Klebsiella sp. UN-79 were studied. The optimal fermentatio -n medium were determined as follows (g/L): glucose 80; yeast extract 20; KH2PO4 6; K2HPO4 15; (NH4)2SO4 3; citrate sodium 4.0; MgSO4·7H2O 0.1; CaCl2 0.05; FeSO4·7H2O 0.005; ZnSO4·7H2O 0.005; MnSO4·7H2O 0.005; EDTA 0.05.3. Effect of various substance on 2,3-butanediol production had been investigated as well. Improvements were observed when acetic acid、ciritic acid、pyruvic acid were added into the medium. Of all acids tested, glycine、alanine of low concentration could enhance the 2,3-butanediol production slightly. Besides, vitamin B1, nicotinic acid could increase the quantity of 2,3-butanediol in fermentation broth. Lower production of 2,3-butanediol was found following the addition of alcohols.4. Fermentation conditons of Klebsiella sp. UN-79 were determined, on the base of the resulting fermentation medium in the shake-flask. The obtained best fermentation condition was described as: original pH5.5-6.5, temperature35℃, amount of inoculation 5%, amount of load 100ml(in 250ml, flask), rotation speed 120rpm for 25h, then standing fermentation for 48h. In addition, the fed-batched cultivations with glucose, alkaline substance were studied. It was found that the quantity of 2,3-butanediol could be improved by continuous additions of glucose and ammonia into the fermentation broth.
Several series of 1,2,3-triazoles containing heterocyclic and naphthalimides compounds were designed and synthesized and their spectra properties,DNA intercalative,antitumor and DNA photo-damaging activities were evaluated.A series of 1,2,3-triazoles fused 1,8-naphthalimide derivatives with electron-deficiency characteristics were designed and synthesized.Their spectra properties,DNA intercalative, DNA photo-damaging and antitumor activities were evaluated.The scatchard binding constant between CT DNA with K1 was monitored by fluorescence spectroscopy technique. The result showed that K1 could effectively intercalate into the CT DNA and the scatchard binding constant reached 105 M-1.Titration CD spectra of CT DNA by K2 illustrated that the mode of K2 interacted with DNA changed from intercalation to aggregation with the concentration of K2 increased.It also revealed that the CT DNA unwound upon K2 intercalation,followed by which the tertiary structure of CT DNA underwent a transition from B-form to A-like conformation.DNA photo-damaging assay showed that these compounds could effectively cleave supercoiled DNA.The antitumor activities test of these compounds exhibited efficient activities against U251,A549 and MOLT-4 cell lines.A series of 6-1,2,3-triazol-1,8-naphthalimide derivatives were designed and synthesized via “Click Chemistry”.Their spectra properties,DNA intercalative,DNA photo-damaging and antitumor activities were evaluated.Titration CD spectra of CT DNA by V2 illustrated that the mode of V2 interacted with DNA changed from intercalation to aggregation with the concentration of V2 increased.It also revealed that the CT DNA unwound upon V2 intercalation,followed by which the tertiary structure of CT DNA underwent a transition from B-form to A-like conformation.DNA photo-damaging assay showed that these compounds could effectively cleave supercoiled DNA.The inhibitory test against A549 and MOLT-4 cell lines in vitro of V2 showed that this compound exhibited high antitumor activities,IC50 of compound V2 against A549 cell reached 0.426μM.A series of 5-1,2,3-triazol-1,8-naphthalimide derivatives were designed and synthesized via “Click Chemistry”.Their spectra properties,DNA intercalative,DNA photo-damaging and antitumor activities were evaluated.The scatchard binding constant between CT DNA with F1 was monitored by fluorescence spectroscopy technique.The result showed that F1 could effectively intercalate into the calf thymus DNA and the scatchard binding constant reached 105 M-1.DNA photo-damaging assay showed that these compounds could effectively cleave supercoiled DNA.The inhibitory test against A549 and MOLT-4 cell lines in vitro of I2 and F2 showed that the compounds exhibited high antitumor activities,especially IC50 of compound F2 against A549 cell reached 0.333μM.These two compound also exhibited high selectivity against A549 and MOLT-4 cell lines.