- Synthesis, characterization and structure-activity relationship analysis of novel depsides as potential antibacterials
[作者:Lv, PC; Xiao, ZP; Fang, RQ; Li, HQ; Zhu, HL; Liu, CH,期刊:European Journal of Medicinal Chemistry, 页码:1779-1787 , 文章类型: Article,,卷期:2009年44-4]
- Twenty-six depsides were synthesized to screen for their antibacterial activity. All of them were reported for the first time. Their chemical structures were clearly determined by H-1 NMR, C-13 NMR, ESI mass spectra and ...
- Design, synthesis and characterization of N-9/N-7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors
[作者:Peifer, C; Buhler, S; Hauser, D; Kinkel, K; Totzke, F; Schachtele, C; Laufer, S,期刊:European Journal of Medicinal Chemistry, 页码:1788-1793 , 文章类型: Article,,卷期:2009年44-4]
- In this study we report on the design, synthesis and biological characterization of novel N-9 or N-7 arylethanone-substituted 6-aminopurines and 6-methoxypurines, respectively, as EGF-R and VEGF-R. inhibitors. The compou...
- Receptor-based 3D-QSAR studies of checkpoint Wee1 kinase inhibitors
[作者:Wichapong, K; Lindner, M; Pianwanit, S; Kokpol, S; Sippl, W,期刊:European Journal of Medicinal Chemistry, 页码:1383-1395 , 文章类型: Article,,卷期:2009年44-4]
- One hundred and seventy-four pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione derivatives reported as inhibitors of the kinase Wee1 were used for a molecular docking and three-dimensional quantitative structure-activity relation...
- Synthesis and in vitro cysticidal activity of new benzimidazole derivatives
[作者:Palomares-Alonso, F; Jung-Cook, H; Perez-Villanueva, J; Piliado, JC; Rodriguez-Morales, S; Palencia-Hernandez, G; Lopez-Balbiaux, N; Hernandez-Campos, A; Castillo, R; Hernandez-Luis, F,期刊:European Journal of Medicinal Chemistry, 页码:1794-1800 , 文章类型: Article,,卷期:2009年44-4]
- Despite albendazole being the drug of choice in neurocysticercosis treatment, its low solubility limits its bioavailability; therefore, more research is required in order to find new molecules with cestocidal activity an...
- Design, synthesis, and anti-tumor evaluation of novel symmetrical bis-benzimidazoles
[作者:Yang, YH; Cheng, MS; Wang, QH; Nie, H; Liao, N; Wang, J; Chen, H,期刊:European Journal of Medicinal Chemistry, 页码:1808-1812 , 文章类型: Article,,卷期:2009年44-4]
- A novel symmetrical bis-benzimidazole was designed as DNA minor groove binder. Molecular modeling study showed that it could dock into the minor groove of DNA. Several derivatives were synthesized and confirmed by IR, MS...
- Antidyslipidemic and antioxidative activities of 8-hydroxyquinoline derived novel keto-enamine Schiffs bases
[作者:Sashidhara, KV; Kumar, A; Bhatia, G; Khan, MM; Khanna, AK; Saxena, JK,期刊:European Journal of Medicinal Chemistry, 页码:1813-1818 , 文章类型: Article,,卷期:2009年44-4]
- 8-Hydroxyquinoline when subjected to Duff reaction resulted in the formation of unexpected 7-methylaminomethylene-8-oxo-7, 8-dihydroquinoline-5-carbaldehyde 2, which existed in the keto-enamine form, in which the aromati...
- Synthesis of novel thiazolone-based compounds containing pyrazoline moiety and evaluation of their anticancer activity
[作者:Havrylyuk, D; Zimenkovsky, B; Vasylenko, O; Zaprutko, L; Gzella, A; Lesyk, R,期刊:European Journal of Medicinal Chemistry, 页码:1396-1404 , 文章类型: Article,,卷期:2009年44-4]
- To examine the anticancer activity several novel thiazolone-based compounds containing 5-aryl-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl framework were obtained. Reaction of 5-aryl-3-phenyl-4,5-dihydropyrazole with 4-thioxo-2-...
- MED-3DMC: A new tool to generate 3D conformation ensembles of small molecules with a Monte Carlo sampling of the conformational space
[作者:Sperandio, O; Souaille, M; Delfaud, F; Miteva, MA; Villoutreix, BO,期刊:European Journal of Medicinal Chemistry, 页码:1405-1409 , 文章类型: Article,,卷期:2009年44-4]
- Obtaining an efficient sampling of the low to medium energy regions of a ligand conformational space is of primary importance for getting insight into relevant binding modes of drug candidates, or for the screening of ri...
- Synthesis and antitumor activity of 6-and 2-(1-substituted-thio-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones
[作者:Zhao, LM; Xie, TP; He, YQ; Xu, DF; Li, SS,期刊:European Journal of Medicinal Chemistry, 页码:1410-1414 , 文章类型: Article,,卷期:2009年44-4]
- In an attempt to develop potent and selective antitumor agents, a series of 6- and 2-(1-substituted-thio-4-methylpent-3-enyl)-5,8-dimethoxynaphthalene-1,4-diones were designed and synthesized. The cytotoxicities of these...
- C-11-labelled PIB analogues as potential tracer agents for in vivo imaging of amyloid beta in Alzheimer's disease
[作者:Serdons, K; Verduyckt, T; Vanderghinste, D; Borghgraef, P; Cleynhens, J; Van Leuven, F; Kung, H; Bormans, G; Verbruggen, A,期刊:European Journal of Medicinal Chemistry, 页码:1415-1426 , 文章类型: Article,,卷期:2009年44-4]
- Pittsburgh Compound-B (PIB) is currently being evaluated clinically for in vivo visualization of amyloid plaques in patients with Alzheimer's disease (AD). We have synthesized three structural isomers of 6-hydroxy-2-(4'-...
- New acyclic nucleosides analogues as potential analgesic, anti-inflammatory, anti-oxidant and anti-microbial derived from pyrimido[4,5-b]quinolines
[作者:El-Gazzar, ABA; Hafez, HN; Nawwar, GAM,期刊:European Journal of Medicinal Chemistry, 页码:1427-1436 , 文章类型: Article,,卷期:2009年44-4]
- Synthesis of 2-thioxopyrimido[4,5-b]quinoline 3a-c by microwave oven was used as a base to synthesis acyclic nucleosides analogue of types, 3-(penta-O-acetyl-glycosyl)-6-(4-chlorophenyl)-10-(4-chlorophenylmethylene)-7,8,...
- Studies on self-aggregation of anthracycline drugs by restrained molecular dynamics approach using nuclear magnetic resonance spectroscopy supported by absorption, fluorescence, diffusion ordered spectroscopy and mass spectrometry
[作者:Agrawal, P; Barthwal, SK; Barthwal, R,期刊:European Journal of Medicinal Chemistry, 页码:1437-1451 , 文章类型: Article,,卷期:2009年44-4]
- Self-association, a process that competes with binding to DNA and formation of hetero-complexes, is studied in anticancer drugs 4'-epiadriamycin, adriamycin and daunomycin by proton nuclear magnetic resonance spectroscop...
- Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities
[作者:Dominguez, JN; Leon, C; Rodrigues, J; de Dominguez, NG; Gut, J; Rosenthal, PJ,期刊:European Journal of Medicinal Chemistry, 页码:1457-1462 , 文章类型: Article,,卷期:2009年44-4]
- The synthesis of novel chlorovinyl sulfone-like chalcone derivatives and their antimalarial activity against cultured Plasmodium falciparum parasites, hemozoin formation, hemoglobin hydrolysis and murine malaria model ar...
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