- A squaraine-based colorimetric and "turn on" fluorescent sensor for selective detection of Hg2+ in an aqueous medium
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A novel squaraine-based chemosensor SQ-1 has been synthesized, and its sensing behavior toward various metal ions was investigated by UV-vis and fluorescence spectroscopies. In AcOH-H2O (40:60, v/v) solution, Hg2+ ions coordinate with SQ-1 causing a deaggregation which induces a visual color and absorption spectral changes as well as strong fluorescence. In contrast, the addition of other metals (e.g., Pb2+, Cd 2+, Cu2+, Zn2+, Al3+, Ni 2+, Co2+, Fe3+, Ca2+, K+, Mg2+, Na+, and Ag+) does not induce these changes at all. Thus SQ-1 is a specific Hg2+ sensing agent due to the inducing deaggregation of the dye molecule by Hg2+.(Figure Presented)
- Chen, Cheng,Wang, Ruyong,Guo, Liangqia,Fu, Nanyan,Dong, Haijun,Yuan, Yaofeng
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Read Online
- Synthesis of hyperbranched azo-polymer-grafted graphene oxide hybrid
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Hyperbranched azo-polymer-grafted graphene oxide (GO) hybrid was synthesized. Epoxy-based precursor polymer was first covalently attached to GO through an ester linkage. Then the hyperbranched azo-polymer-grafted graphene oxide hybrid can be obtained by azo-coupling reaction between the epoxybased precursor-polymer-functionalized GO and hyperbranched diazonium salts under extremely mild conditions.
- Wang, Yang,Wei, Renbo,He, Yaning,Wang, Xiaogong
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Read Online
- Hypoxia-activatable nano-prodrug for fluorescently tracking drug release in mice
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Chemotherapy is one of the commonly used methods to treat various types of cancers in clinic by virtue of its high efficiency and universality. However, strong side effects and low concentration of conventional drugs at the tumor site have always been important factors that plague the chemotherapy effects of patients, further precluding their practical applications. Thereof, to solve the above dilemma, by integration of anticancer drug (nitrogen mustard, NM) into an NIR fluorophore (a dicyanoisophorone derivative), an intelligent prodrug NIR-NM was developed via molecular engineering strategy. Prodrug NIR-NM stimulated in hypoxia condition exhibits significantly higher toxicity to cancer cells than normal cells, essentially reducing the collateral damage to healthy cells and tissues of nitrogen mustard. More importantly, the nanoparticle prodrug FA-lip@NIR-NM showed the advantages of the high accumulation of drug at tumor site and long-circulation capacity in vivo, which endowed it the ability to track the release of the active chemotherapeutic drug and further treat solid tumors.[Figure not available: see fulltext.].
- Li, Haidong,Yao, Qichao,Pu, Zhongji,Chung, Jeewon,Ge, Haoying,Shi, Chao,Xu, Ning,Xu, Feng,Sun, Wen,Du, Jianjun,Fan, Jiangli,Wang, Jingyun,Yoon, Juyoung,Peng, Xiaojun
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p. 499 - 508
(2021/01/25)
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- Fluorescent probe molecule for detecting azo reductase based on coumarin derivative as well as preparation method and application of fluorescent probe molecule
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The invention provides a fluorescent probe molecule for detecting azo reductase based on a coumarin derivative as well as a preparation method and application of the fluorescent probe molecule, and belongs to the technical field of protease detection reagents. The fluorescent probe molecule prepared by the invention can provide a molecule combined with a specific biological enzyme-azo reductase, so that azo groups in a probe structure are reduced by the azo reductase, a fluorophore coumarin derivative is released, fluorescence of the probe molecule is changed, and an anticancer active drug phenylalanine mustard is released at the same time; therefore, the azo reductase in a liquid phase system is selectively identified and detected. Therefore, the invention provides the application of the fluorescent probe molecule in preparation of a reagent for detecting azo reductase and/or detection of Sn in a water body.
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Paragraph 0083; 0087
(2021/07/17)
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- Fluorescent probe for detecting tiredness level Preparation method and application thereof
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The invention discloses a fluorescence probe for detecting the level of hypoxia, a preparation method and application thereof, and can realize specific response Na. 2 S2 O4 The fluorescence probe is used for detecting the tiredness level, and the structure is as follows. The probe comprises a nitrogen-nitrogen double bond, which can be broken down in a hypoxic environment to cause fluorescence recovery of the compound. The naphthalimide is introduced as a fluorophore, and has the characteristics of stable fluorescence and high fluorescence quantum efficiency. The fluorescent probe is simple and convenient to prepare, obvious in spectral change, good in specificity effect, small in cytotoxicity, good in imaging effect and good in specificity detection Na. 2 S2 O4 , The fluorophore precursor and the anti-tumor drug nitrogen mustard compound can be released under the hypoxic condition, the tumor cell growth can be inhibited while the hypoxia imaging is carried out, the diagnosis and treatment integrated function is achieved, and the application prospect is good.
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Paragraph 0044; 0056-0058
(2021/09/08)
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- Synergetic activation of CO2by the DBU-organocatalyst and amine substrates towards stable carbamate salts for synthesis of oxazolidinones
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The development of an efficient methodology to transform CO2 into valuable chemicals has attracted increasing attention concerning the challenging issues of CO2-utilization. Herein, an efficient approach for the preparation of oxazolidinones from CO2, primary (aliphatic/aromatic) amines and 1,2-dichloroethane (or its derivatives) catalyzed by DBU organo-superbase was achieved with yields of 47-97% under mild conditions (80-100 °C, 12 h, 1.0 MPa CO2). Control experiments demonstrated that the formation of an ion-pair carbamate salt intermediate IS-B derived from the reaction of CO2, DBU (catalyst) and an amine (substrate) was the key step for this three-component reaction. The available DBU-amine-CO2 adduct intermediate (like IS-B-2) with fair stability will evolve into the thermodynamically stable product oxazolidinones upon attack of 1,2-dichloroethane (or its derivatives), along with the regeneration of the DBU catalyst. Alternatively, the decomposition of the DBU-aryl amine-CO2 adduct (like IS-B-1) with relatively poor stability also could result in the competitive substitution reaction of 1,2-dichloroethane (or its derivatives) with the aryl amine. This work provides insights into synergetic CO2-activation by the DBU-catalyst and a nucleophilic amine-substrate via the formation of robust carbamate salt intermediates responsible for the final production of oxazolidinones. This journal is
- Chen, Xiao-Chao,Liu, Ye,Lu, Yong,Yao, Yin-Qing,Zhao, Kai-Chun
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p. 7072 - 7082
(2021/11/17)
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- Chemoselective detection of Ag+ in purely aqueous solution using fluorescence ‘turn-on’ probe based on crown-containing 4-methoxy-1,8-naphthalimide
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A novel derivative of 4-methoxy-1,8-naphthalimide bearing N-phenylazadithia-15-crown-5 ether receptor has been demonstrated as the selective and sensitive fluorescent probe for the detection of silver(I) ions in purely aqueous solution at neutral pH.
- Panchenko, Pavel A.,Polyakova, Anna S.,Fedorov, Yurii V.,Fedorova, Olga A.
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p. 155 - 157
(2019/04/25)
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- Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents
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We describe several new aromatic nitrogen mustards with various aromatic substituents and boronic esters that can be activated with H2O2 to efficiently cross-link DNA. In vitro studies demonstrated the anticancer potential of these compounds at lower concentrations than those of other clinically used chemotherapeutics, such as melphalan and chlorambucil. In particular, compound 10, bearing an amino acid ester chain, is selectively cytotoxic toward breast cancer and leukemia cells that have inherently high levels of reactive oxygen species. Importantly, 10 was 10-14-fold more efficacious than melphalan and chlorambucil for triple-negative breast-cancer (TNBC) cells. Similarly, 10 is more toxic toward primary chronic-lymphocytic-leukemia cells than either chlorambucil or the lead compound, 9. The introduction of an amino acid side chain improved the solubility and permeability of 10. Furthermore, 10 inhibited the growth of TNBC tumors in xenografted mice without obvious signs of general toxicity, making this compound an ideal drug candidate for clinical development.
- Chen, Wenbing,Fan, Heli,Balakrishnan, Kumudha,Wang, Yibin,Sun, Huabing,Fan, Yukai,Gandhi, Varsha,Arnold, Leggy A.,Peng, Xiaohua
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p. 9132 - 9145
(2018/10/20)
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- Preparation method of anti-tumor medicine chlorambucil
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The invention belongs to the field of compound preparation, and specifically discloses a preparation method of an anti-tumor medicine chlorambucil. The preparation method comprises the steps of performing a Vilsmeier reaction on a raw material N,N-dihydroxyethylaniline and phosphorus oxychloride and DMF so as to prepare 4-[bi(2-chloroethyl)amino]benzaldehyde, then performing a witting reaction on4-[bi(2-chloroethyl)amino]benzaldehyde and methoxymethyl triphenylphosphonium chloride so as to prepare 4-[bi(2-chloroethyl)amino]-BETA-methoxystyrene, reacting under an acid condition so as to obtain4-[bi(2-chloroethyl)amino]phenylacetaldehyde, and finally, reacting with Meldrum's acid in triethylamine and formic acid systems so as to prepare a target product. The raw material N,N-dihydroxyethylaniline is cheap, has a wide source and is easy to obtain; the whole reaction process has high yield, production conditions are mild, the steps are short, and post treatment and purification are easyto operate, so that the preparation method is applicable to commercial large scale production, and meets the rapidly growing market demands.
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Paragraph 0024; 0036; 0040; 0041; 0042
(2018/03/28)
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- A hypoxia-specific and mitochondria-targeted anticancer theranostic agent with high selectivity for cancer cells
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Herein, a novel soluble mitochondria-targeted theranostic compound, HMX-1, was presented, which was selectively activated under hypoxia with excellent mitochondria-targeting ability at the cellular level, accompanied by a dramatic increase in the fluorescence intensity. Moreover, its anti-cancer efficiency was certified both in vitro and in vivo.
- Hu, Mingxing,Yang, Chao,Luo, Yi,Chen, Fan,Yang, Fangfang,Yang, Shuping,Chen, Hao,Cheng, Zhiqiang,Li, Kun,Xie, Yongmei
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supporting information
p. 2413 - 2416
(2018/05/04)
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- A copper ion Schiff base probe compound and its preparation method (by machine translation)
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The invention provides a copper ion Schiff-base probe compound adopting the structure shown in the formula I and a preparation method thereof. The preparation method comprises steps as follows: firstly, Rhodamine hydrazide is prepared from Rhodamine B and hydrazine hydrate, then N,N-dichloroethylaniline is prepared from N,N-dihydroxyethylaniline and reacts with DMF (dimethylformamide) and POCl3 for preparation of N,N-dichloroethylbenzaldehyde, finally, the N,N-dichloroethylbenzaldehyde reacts with the Rhodamine hydrazide, and the Schiff-base probe compound is obtained. The copper ion Schiff-base probe compound shows specific selectivity for copper ions in a buffer solution, the copper ions can be identified under the condition of observation with naked eyes, and the compound can be widely applied to detection of content of silver in animals, plants, human cells, soil or water bodies.
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Paragraph 0022; 0041
(2018/02/04)
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- Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies
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Malaria deaths have been decreasing over the last 10-15 years, with global mortality rates having fallen by 47% since 2000. While the World Health Organization (WHO) recommends the use of artemisinin-based combination therapies (ACTs) to combat malaria, the emergence of artemisinin resistant strains underscores the need to develop new antimalarial drugs. Recent in vivo efficacy improvements of the historical antimalarial ICI 56,780 have been reported, however, with the poor solubility and rapid development of resistance, this compound requires further optimization. A series of piperazine-containing 4(1H)-quinolones with greatly enhanced solubility were developed utilizing structure-activity relationship (SAR) and structure-property relationship (SPR) studies. Furthermore, promising compounds were chosen for an in vivo scouting assay to narrow selection for testing in an in vivo Thompson test. Finally, two piperazine-containing 4(1H)-quinolones were curative in the conventional Thompson test and also displayed in vivo activity against the liver stages of the parasite.
- Neelarapu, Raghupathi,Maignan, Jordany R.,Lichorowic, Cynthia L.,Monastyrskyi, Andrii,Mutka, Tina S.,LaCrue, Alexis N.,Blake, Lynn D.,Casandra, Debora,Mashkouri, Sherwin,Burrows, Jeremy N.,Willis, Paul A.,Kyle, Dennis E.,Manetsch, Roman
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p. 1450 - 1473
(2018/03/05)
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- An azobenzene-based heteromeric prodrug for hypoxia-activated chemotherapy by regulating subcellular localization
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An azobenzene-based heteromeric prodrug (hNDP) was prepared for targeted chemotherapy against hypoxic tumor. hNDP could divert the parent drug from nucleus to cytoplasm with lower toxicity, while the azoreduction of hNDP in hypoxia would activate the drug with a robust anti-tumor effect by initiating the apoptosis-related biochemical cascades.
- Li, Shiying,Jiang, Xueyan,Zheng, Rongrong,Zuo, Shengjia,Zhao, Linping,Fan, Guiling,Fan, Jinghao,Liao, Yonghua,Yu, Xiyong,Cheng, Hong
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supporting information
p. 7983 - 7986
(2018/07/25)
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- Quinolone-based compounds, formulations, and uses thereof
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Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.
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Page/Page column 61
(2018/07/02)
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- Hypoxia activation doxorubicin prodrug and preparation method thereof
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The invention discloses a hypoxia activation doxorubicin prodrug and a preparation method thereof. The doxorubicin prodrug is synthesized by modification of an amino group located at a 3' position ofdoxorubicin by an azo bond having a hypoxia activation effect and a response functional group having a self-occluded structure. The doxorubicin prodrug provided by the invention can effectively realize selective activation under a hypoxic environment, and can regulate and control growth activity of tumor cells by regulating subcellular organelle distribution of the doxorubicin in normoxia and hypoxic environments, thereby reducing toxic and side effects of a drug on normal cells, improving targeting efficiency of the drug on tumor treatment, and providing more novel ideas for development of antitumor drugs; and the synthetic method for the hypoxia activation doxorubicin prodrugs provided by the invention is simple, raw materials are cheap and easy to obtain, and the hypoxia activation doxorubicin prodrugs are convenient for industrialized production and clinical transformation.
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Paragraph 0041; 0043; 0045-0047
(2018/09/08)
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- METALLOENZYME INHIBITOR COMPOUNDS
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Provided are compounds having HDAC6 modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by HDAC6.
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Page/Page column 147
(2018/09/28)
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- Synthesis, characterization and theoretical investigations of molybdenum carbonyl complexes with phosphorus/nitrogen/phosphorus ligand as bidentate and tridentate modes
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Carbonyl complexes of molybdenum with the phosphorus/nitrogen/phosphorus ligand, PNP-Mo(CO)n, where n = 3, 4 and PNP is N,N-bis[2-(diphenylphosphino)ethyl]phenylamine have been synthesized and characterized by 1H, 31P{1H} NMR, IR (ATR and solution state), Raman, X-ray diffraction, MS and elemental analysis. DFT calculations of the complexes were also performed. The PNP-Mo(CO)4 complex in which the binding mode is bidentate cis-phosphine and, facial and meridional isomers of PNP-Mo(CO)3 in which the binding mode is tridentate were obtained. The facial isomer and the tetracarbonyl complexes were successfully synthesized and purified; however, it was not possible to isolate the meridional isomer. Only a few crystals of the meridional isomer were detected and used for X-ray analysis. When the facial isomer was dissolved in CH2Cl2 or in THF, it was found to undergo decomposition thereby generating the tetracarbonyl complex, meridional isomer, Mo(0) as a dark precipitate along with some facial isomer that was left intact in solution. The reason that the facial isomer was the preferred structure with respect to the meridional isomer was also investigated.
- Goren Keskin, Seyma,Stanley, Julie M.,Cowley, Alan H.
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p. 206 - 217
(2017/10/16)
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- A Bis-Quinoline Appended Azobenzene Based Naked Eye Sensor for Selective Detection of Cd2+ Ion
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A new azobenzene chromophore (AZQU), appended with a bis-quinoline unit as a turn-on chemosensor for selective detection of Cd2+ ions, has been designed and synthesized. The fluorescent receptor AZQU has an excellent selectivity and sensitivity towards Cd2+ ions over other metal ions in CH3CN:H2O (80:20, v/v) solution. AZQU is red colored and non-fluorescent in the absence of Cd2+ ions, but upon addition of Cd2+ ions it turns colorless with appreciable fluorescence. This “off–on” type signaling behavior is attributed to the CHEF (chelation-enhanced fluorescence) effect of the quinoline unit and the change in color from red to yellow occurs by an ICT process with Cd2+. The association constant for AZQU?+?Cd2+ was calculated to be 1.68?×?105 L·mol?1 with binding in the 1:1 stoichiometric ratio.
- Hrishikesan, Elango,Manjunath, Rangasamy,Kannan, Palaninathan
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p. 907 - 919
(2016/07/06)
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- Synthesis, characterization, and antitumor activity of rare earth metal complexes of benzoic acid nitrogen mustard
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Benzoic acid nitrogen mustard and its rare earth metal complexes were synthesized and characterized by elemental analyses, IR, electronic spectrum, and EPR. The interaction of synthesized complexes with Ct-DNA was investigated and reviewed as a mixed manner of both intercalation and alkylation via fluorescence titration. Their biological activities were also evaluated in K562 and Vero cell lines, indicating that complexes had a significant inhibitory effect; however, there was no synergistic effect instead of antagonistic effect compared to benzoic acid nitrogen mustard. The possible mechanism through cellular apoptosis was also explored by comet assay.
- Zhou, Sufeng,Fu, Yun,Fan, Xizhi,Zhang, Yanfang,Li, Changzheng
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p. 2862 - 2869
(2013/07/26)
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- Siloxane polymers containing azo moieties synthesized by click chemistry for photo responsive and liquid crystalline applications
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Three new types of siloxane-based photoactive liquid crystalline polymers containing azo side groups were synthesized through the click chemistry route. The polymers having molecular weight range of 14,000-34,000 g mol-1 were soluble in most of the polar solvents like chloroform, tetrahydrofuran, dimethylformamide, dimethyl sulfoxide, and dichloromethane. The photoresponsive trans-cis photoisomerization under UV radiation and cis-trans relaxation process in dark for the polymers were studied. The isomerization rate constants were found to be 0.01-0.04 sec-1 and 1.16*10-4-4. 67*10-4 sec-1, respectively. It has been noted that the polymers showed high intensity absorption for n-π* in chloroform. Both trans and cis forms of azide monomers having azo moiety exhibited molar extinction coefficient (Iμmax) in the range of 22,000-33,000 L mol-1 cm-1. The thermotropic behavior of the polymers was studied by polarizing optical microscope (POM) and differential scanning calorimetry (DSC) experiments. Polymer P1 showed liquid crystalline textures of nematic droplets, whereas P2 showed smectic focal conic texture and nematic droplets. Polymer P1 was also studied for photomechanical bending on exposure to UV radiation. The polymers showed initial degradation temperature in the range of 210-275°C.
- Pandey, Someshwarnath,Kolli, Balakrishna,Mishra, Sarada P.,Samui, Asit B.
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scheme or table
p. 1205 - 1215
(2012/06/01)
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- Hyperbranched photo responsive and liquid crystalline azo-siloxane polymers synthesized by click chemistry
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Three new types of hyperbranched photoactive liquid crystalline siloxane polymers containing azo moieties were synthesized using click chemistry methodology. The polymers were soluble in most of the polar solvents like chloroform, tetrahydrofuran, dimethylformamide, dimethyl sulphoxide and dichloromethane. The molecular weights of the polymers were in the range of 9000-12,000 g mol-1. The trans-cis photoisomerization of the polymer were studied both under UV radiation and dark. The isomerization rate constants were found to be in the range of 0.7-1.4 × 10-2 sec -1 and 7.0 × -2.5 × 10-5 sec-1. The thermotropic behavior of the polymers was studied by using polarizing optical microscopy and differential scanning calorimetry, respectively. The polymers P1 and P2 showed liquid crystalline texture characteristic of nematic phase.
- Pandey, Someshwarnath,Mishra, Sarada P.,Kolli, Balakrishna,Kanai, Tapan,Samui, Asit B.
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scheme or table
p. 2659 - 2668
(2012/08/13)
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- Click chemistry-based synthesis of azo polymers for second-order nonlinear optics
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Four linear polymers containing pendant azo moiety were synthesized through click chemistry for second-order nonlinear optical study. The polymers were found soluble in most of the polar organic solvents such as tetrahydrofuran (THF), chloroform, and dimethyl formamide (DMF). The polymers showed thermal stability up to 300 °C and glass transition temperatures (Tg) in the range of 120-140 °C. The molecular weights (Mw) of these polymers (measured by gel permeation chromatography) were in the range 37,900-55,000 g/mol. The polymers were found to form optically transparent films by solution casting from THF solution. Order parameters were calculated from UV-vis absorption spectra. The morphology changes in the films after poling were characterized by atomic force microscopy. The angular dependence, temperature dependence, and time dependence of second harmonic generation (SHG) intensity were obtained by using 1064 nm Nd:YAG laser. The SHG intensity remained unchanged up to 95 °C. At room temperature, it remained stable up to 8 days after initial drop of about 14%.
- Kolli, Balakrishna,Mishra, Sarada P.,Joshi,Raj Mohan,Dhami,Samui
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scheme or table
p. 1572 - 1578
(2012/06/01)
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- Synthesis and structure-analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ)
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A series of monospirocyclopiperazinium salts were designed and synthesized to search for a peripherally-acting analgesic drug with low side effects. Extensive SAR studies revealed that a suitable NR2R3 was critical for the analgesic activity, which might be beneficial to expose the cationic nitrogen to bind to the receptor, and possibly interact with the receptor via π-π interaction. Introduction of substituting group on the N4-phenyl ring could improve the activity, and the best position was the 4-position. Compound 14n showed more potent analgesic activity (63%, 20 μM/kg, sc) and holds promise for development as a mechanically new analgesic drug.
- Lin, Song-Wen,Sun, Qi,Ge, Ze-Mei,Wang, Xin,Ye, Jia,Li, Run-Tao
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p. 940 - 943
(2011/03/21)
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- COMPOUNDS AND USES THEREOF
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There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.
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Page/Page column 36; Sheet 8/19
(2008/12/05)
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- Synthesis, complexation, and E-Z photoisomerization of azadithiacrown- containing styryl dyes as new optical sensors for mercury cations
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New styryl dyes containing azadithia-15-crown-5 fragments were synthesized. The complexation of these compounds with Ag+, Pb2+, Cu2+, Hg2+, and H+ cations was studied by 1H NMR spectroscopy, steady-state, and time-resolved spectroscopy. The stability constants of the complexes were calculated from the spectrophotometric titration data. The photophysical properties and E-Z photoisomerization of styryl dyes and their complexes with mercury and copper(II) cations in acetonitrile were examined.
- Tulyakova,Fedorova,Fedorov,Jonusauskas,Kuz'Mina,Howard,Anisimov
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p. 513 - 526
(2008/03/28)
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- NOVEL SULFONAMIDE DERIVATIVE
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A compound of the formula (1): wherein m, n and p is independently an integer of 0 to 4 with the proviso that 3 a?| m + n a?| 8; X is the formula: NR4, etc.; R1, R3 and R4 are a substituted or unsubstituted aryl group, etc.; R2 is a hydrogen atom, etc.; a, b, c, d, e and f are a hydrogen atom or a substituted or unsubstituted alkyl group, etc.; Y is the formula: -SO2-, etc.; and Z is an oxygen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt of the same has an activity of potentiating an expression of a low density lipoprotein receptor and thus is useful as an agent for treating hyperlipidemia or arteriosclerosis.
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Page/Page column 52-53
(2010/11/25)
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- NOVEL PIPERIDINE DERIVATIVE
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The invention provides a compound of the following formula (1): wherein m, n, and p are independently an integer of 0 - 4, provided 3 ≤ m + n ≤ 8; X is nitrogen atom or a group of the formula: C-R15; Y is a substituted or unsubstituted aromatic group, etc.; R15, R1, R2, R3, R4 , R5, R6 and R7 are hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and Z is hydrogen atom, cyano group, etc., or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which exhibits an action for enhancing LDL receptor expression, and is useful as a medicament for treating hyperlipidemia, atherosclerosis, etc.
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Page/Page column 41
(2008/06/13)
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- Synthesizing hyperbranched azo polymer through azo-coupling reaction
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An AB2 monomer N,N-bis[2-(4-aminobenzoyloxy)ethyl]-aniline was synthesized by nucleophilic substitution reaction between N,N-bis(2-chloroethyl) aniline and 4-aminobenzonic acid. Based on the monomer, the azo-coupling reaction was explored for the first time to prepare a hyperbranched azo polymer. The results showed that the scheme was a feasible way to synthesize hyperbranched azo polymers under extremely mild conditions.
- Che, Pengchao,He, Yaning,Zhang, Yue,Wang, Xiaogong
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- Potassium iodide catalysed monoalkylation of anilines under microwave irradiation
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A potassium iodide catalysed method for the selective N-monoalkylation anilines with alkylhalides and alkyltosylates under microwave irradiation is described. The corresponding N-alkylanilines are obtained in good yields with only minor quantities of dialkylation by-products.
- Romera, Juan L.,Cid, José M.,Trabanco, Andrés A.
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p. 8797 - 8800
(2007/10/03)
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- Inhibition of HIV integrase by 4-hydroxycoumarin dimer bearing aniline mustard moiety
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The design, synthesis of novel HIV-integrase (HIV-IN) inhibitors possessing the 4-hydroxycoumarin dimer bearing aniline mustard moiety are described. These compounds showed good inhibitory activity against HIV-IN.
- Mao, Pili Chih-Min,Mouscadet, Jean-Francois,Leh, Herve,Auclair, Christian,Hsu, Ling-Yih
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p. 1263 - 1270
(2007/10/03)
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- Hypoxia-Selective Antitumor Agents. 3. Relationships between Structure and Cytotoxicity against Cultured Tumor Cells for Substituted N,N-Bis(2-chloroethyl)anilines
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A series of aniline mustards with a wide range of electron-donating and -withdrawing substituents in the 3- and 4-positions has been synthesized and evaluated for cytotoxicity in cell culture to examine the potential of using nitro group deactivated nitrogen mustards for the design of novel hypoxia-selective anticancer drugs (Denny, W.A.; Wilson, W.R.J.Med Chem. 1986, 29, 879).Hydrolytic half-lives in tissue culture media, determined by bioassay against a cell line (UV4) defective in the repair of DNA interstrand cross-links showed the expected dependence on the Hammett electronic parameter, ?, varying from 0.13 h for the 4-amino analogue to >100 h for analogues with strongly electron-withdrawing substituents.Cytotoxic potencies in aerobic UV4 cultures showed a similar dependence on ?.This dependence predicted that the 4-nitroaniline mustard would be 7200-fold less potent than its potential six-electron reduction product, the 4-amino compound, in growth inhibition assays using a 1-h drug exposure.The measured differential was much lower (225-fold) because of the instability of the latter compound, but a differential of 17500-fold was observed in the initial rate of killing by using a clonogenic assay.The potential for formation of reactive mustards by reduction to the amine or hydroxylamine was demonstrated by the 4-nitroso compound, which had an aerobic toxicity similar to that of the amine.Although these features confirmed the original rationale, the 3-nitro- and 4-nitroaniline mustards had only minimal hypoxic selectivity against UV cells.Toxicity to hypoxic cells appears to be limited by the low reduction potentials of these compounds and consequent lack of enzymatic nitroreduction.However, this study has demonstrated that nitro groups can be used to latentiate aromatic nitrogen mustards and indicates that examples with higher reduction potentials could provide useful hypoxia-selective therapeutic agents.
- Palmer, Brian D.,Wilson, William R.,Pullen, Susan M.,Denny, William A.
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p. 112 - 121
(2007/10/02)
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- THE EFFECTS OF CYCLIC TERMINAL GROUPS IN 4-AMINOAZOBENZENE AND RELATED AZO DYES. PART 3. ELECTRONIC ABSORPTION SPECTRA OF SOME MONOAZO DYES DERIVED FROM N-PHENYLMORPHOLINE, N-(PHENYL)THIOMORPHOLINE, N-(PHENYL)THIOMORPHOLINE 1,2-DIOXIDE, AND N-ACETYL-N'-PHENYLPIPERAZINE
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Monoazo dyes containing a terminal morpholino group absorp hypsochromically in comparison with their piperidino counterparts as a result of electron withdrawal by the oxygen atom.Similar shifts are observed with related dyes possessing other γ-heteroatoms in the donor group.In acid solution, protonation takes place at the β-azo nitrogen atom (azonium tautomer) and at the terminal nitrogen atom (ammonium tautomer) to an extent which depends on the inductive effect of the γ-substituent.
- Hallas, Geoffrey,Marsden, Richard,Hepworth, John D.,Mason, Donald
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p. 123 - 126
(2007/10/02)
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