- Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors (Retraction of vol 35, pg 909, 2010)
[作者:Sahoo, PK; Behera, P,期刊:European Journal of Medicinal Chemistry, 页码:5225-5225 , 文章类型: Correction,,卷期:2011年46-10]
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- Biophysical and physicochemical methods differentiate highly ligand-efficient human D-amino acid oxidase inhibitors
[作者:Lange, JHM; Venhorst, J; van Dongen, MJP; Frankena, J; Bassissi, F; de Bruin, NMWJ; den Besten, C; de Beer, SBA; Oostenbrink, C; Markova, N; Kruse, CG,期刊:European Journal of Medicinal Chemistry, 页码:4808-4819 , 文章类型: Article,,卷期:2011年46-10]
- Many early drug research efforts are too reductionist thereby not delivering key parameters such as kinetics and thermodynamics of target ligand binding. A set of human D-Amino Acid Oxidase (DAAO) inhibitors 1-6 was appl...
- Synthesis, stereochemistry and SAR of a series of minodronate analogues as RGGT inhibitors
[作者:Blazewska, KM; Ni, F; Haiges, R; Kashemirov, BA; Coxon, FP; Stewart, CA; Baron, R; Rogers, MJ; Seabra, MC; Ebetino, FH; McKenna, CE,期刊:European Journal of Medicinal Chemistry, 页码:4820-4826 , 文章类型: Article,,卷期:2011年46-10]
- Phosphonocarboxylate (PC) analogues of bisphosphonates are of interest due to their selective inhibition of a key enzyme in the mevalonate pathway, Rab geranylgeranyl transferase (RGGT). The dextrarotatory enantiomer of ...
- Synthesis and antitubercular evaluation of novel dibenzo[b,d]furan and 9-methyl-9H-carbazole derived hexahydro-2H-pyrano[3,2-c]quinolines via Povarov reaction
[作者:Kantevari, S; Yempala, T; Surineni, G; Sridhar, B; Yogeeswari, P; Sriram, D,期刊:European Journal of Medicinal Chemistry, 页码:4827-4833 , 文章类型: Article,,卷期:2011年46-10]
- A series of novel hexahydro-2H-pyrano[3,2-c]quinoline analogues derived from dibenzo[b,d]furan and 9-methyl-9H-carbazole has been synthesized in very good yields through SnCl(2)center dot 2H(2)O catalyzed one-pot Povarov...
- Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties
[作者:Thomas, KD; Adhikari, AV; Chowdhury, IH; Sandeep, T; Mahmood, R; Bhattacharya, B; Sumesh, E,期刊:European Journal of Medicinal Chemistry, 页码:4834-4845 , 文章类型: Article,,卷期:2011年46-10]
- New series of quinoline-oxazolidinone hybrid molecules were synthesized based on the preliminary docking studies. All the newly synthesized compounds were characterized by spectral analyses. The newly synthesized compoun...
- Synthesis and selective human monoamine oxidase inhibition of 3-carbonyl, 3-acyl, and 3-carboxyhydrazido coumarin derivatives
[作者:Secci, D; Carradori, S; Bolasco, A; Chimenti, P; Yanez, M; Ortuso, F; Alcaro, S,期刊:European Journal of Medicinal Chemistry, 页码:4846-4852 , 文章类型: Article,,卷期:2011年46-10]
- Several 3-carbonyl (1-26), 3-acyl (27-52), and 3-carboxyhydrazido (53-58) coumarins have been synthesized in high yields (72-99%) and tested in vitro for their human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibito...
- Thiazolyl N-benzyl-substituted acetamide derivatives: Synthesis, Src kinase inhibitory and anticancer activities
[作者:Fallah-Tafti, A; Foroumadi, A; Tiwari, R; Shirazi, AN; Hangauer, DG; Bu, YH; Akbarzadeh, T; Parang, K; Shafiee, A,期刊:European Journal of Medicinal Chemistry, 页码:4853-4858 , 文章类型: Article,,卷期:2011年46-10]
- KX2-391 (KX-01/Kinex Pharmaceuticals), N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl) acetamide, is a highly selective Src substrate binding site inhibitor. To understand better the role of pyridine ring and N...
- Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: Perhydropyrrole[1,2-a]pyrazines
[作者:Dawidowski, M; Herold, F; Chodkowski, A; Kleps, J; Szulczyk, P; Wilczek, M,期刊:European Journal of Medicinal Chemistry, 页码:4859-4869 , 文章类型: Article,,卷期:2011年46-10]
- A number of novel pyrrole[1,2-a]pyrazine derivatives were synthesized and evaluated in in vivo animal models of epilepsy. Among them, several compounds displayed promising seizure protection in the maximal electroshock s...
- Development of a novel furocoumarin derivative inhibiting NF-kappa B dependent biological functions: Design, synthesis and biological effects
[作者:Borgatti, M; Chilin, A; Piccagli, L; Lampronti, I; Bianchi, N; Mancini, I; Marzaro, G; dall'Acqua, F; Guiotto, A; Gambari, R,期刊:European Journal of Medicinal Chemistry, 页码:4870-4877 , 文章类型: Article,,卷期:2011年46-10]
- Nuclear Factor kappaB (NF-kappa B) plays a very important role in the control of gene expression and is deeply involved in several human pathologies. Accordingly, molecules targeting NF-kappa B dependent biological funct...
- Synthesis and characterization of novel PUFA esters exhibiting potential anticancer activities: An in vitro study
[作者:Khan, AA; Alam, M; Tufail, S; Mustafa, J; Owais, M,期刊:European Journal of Medicinal Chemistry, 页码:4878-4886 , 文章类型: Article,,卷期:2011年46-10]
- Polyunsaturated fatty acids (PUFAs) have been reported to play a regulatory role in tumour growth progression. In the present study, we have synthesized ester derivatives of two important PUFA viz., linoleic acid (LA) an...
- Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents
[作者:Rajitha, C; Dubey, PK; Sunku, V; Piedrafita, FJ; Veeramaneni, VR; Pal, M,期刊:European Journal of Medicinal Chemistry, 页码:4887-4896 , 文章类型: Article,,卷期:2011年46-10]
- The synthesis of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives has been carried out using trifluoroacetic anhydride/phosphoric acid mediated C C bond forming reaction as a key step. This method does not require the ...
- Synthesis of 3-heteroarylthioquinoline derivatives and their in vitro antituberculosis and cytotoxicity studies
[作者:Chitra, S; Paul, N; Muthusubramanian, S; Manisankar, P; Yogeeswari, P; Sriram, D,期刊:European Journal of Medicinal Chemistry, 页码:4897-4903 , 文章类型: Article,,卷期:2011年46-10]
- A series of 3-heteroarylthioquinoline derivatives has been synthesized by the Friedlander annulation of 2-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]-1-aryl-1-ethanone/2-(1,3-benzothiazol-2-ylsulfanyl)-1-aryl-1-ethanone/1...
- Tyrosyl-tRNA synthetase inhibitors as antibacterial agents: Synthesis, molecular docking and structure-activity relationship analysis of 3-aryl-4-arylaminofuran-2(5H)-ones
[作者:Xiao, ZP; Ma, TW; Liao, ML; Feng, YT; Peng, XC; Li, JL; Li, ZP; Wu, Y; Luo, Q; Deng, Y; Liang, X; Zhu, HL,期刊:European Journal of Medicinal Chemistry, 页码:4904-4914 , 文章类型: Article,,卷期:2011年46-10]
- Thirty-five 3-aryl-4-arylaminofuran-2(5H)-one derivatives were designed, prepared and tested for their inhibitory activity against tyrosyl-tRNA synthetase. Out of these compounds, 3-(3-bromophenyl)-4-(3,5-dichlorophenyla...
- Overcoming human P-glycoprotein-dependent multidrug resistance with novel dihydro-beta-agarofuran sesquiterpenes
[作者:Perestelo, NR; Sanchez-Canete, MP; Gamarro, F; Jimenez, IA; Castanys, S; Bazzocchi, IL,期刊:European Journal of Medicinal Chemistry, 页码:4915-4923 , 文章类型: Article,,卷期:2011年46-10]
- Sixteen (1-16) dihydro-beta-agarofuran sesquiterpenes were isolated from the fruits of Maytenus jelskii and evaluated against mammalian cells with a multidrug resistance phenotype mediated by the overexpression of the hu...
- Anti-AIDS agents 86. Synthesis and anti-HIV evaluation of 2 ',3 '-seco-3 '-nor DCP and DCK analogues
[作者:Chen, Y; Cheng, M; Liu, FQ; Xia, P; Qian, KD; Yu, DL; Xia, Y; Yang, ZY; Chen, CH; Morris-Natschke, SL; Lee, KH,期刊:European Journal of Medicinal Chemistry, 页码:4924-4936 , 文章类型: Article,,卷期:2011年46-10]
- In a continuing study of novel anti-HIV agents with drug-like structures and properties, 30 1'-O-, 1'-S-, 4'-O- and 4'-substituted-2',3'-seco-3'-nor DCP and DCK analogues (8-37) were designed and synthesized. All newly s...
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