- Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: Design, synthesis, structure-activity relationships, physicochemical properties and biological activity
[作者:Blaazer, AR; Lange, JHM; van der Neut, MAW; Mulder, A; den Boon, FS; Werkman, TR; Kruse, CG; Wadman, WJ,期刊:European Journal of Medicinal Chemistry, 页码:5086-5098 , 文章类型: Article,,卷期:2011年46-10]
- The discovery, synthesis and structure-activity relationship (SAR) of a novel series of cannabinoid 1 (CB(1)) and cannabinoid 2 (CB(2)) receptor ligands are reported. Based on the aminoalkylindole class of cannabinoid re...
- Ruthenium(II) phosphine/diimine/picolinate complexes: Inorganic compounds as agents against tuberculosis
[作者:Pavan, FR; Poelhsitz, GV; Barbosa, MIF; Leite, SRA; Batista, AA; Ellena, J; Sato, LS; Franzblau, SG; Moreno, V; Gambino, D; Leite, CQF,期刊:European Journal of Medicinal Chemistry, 页码:5099-5107 , 文章类型: Article,,卷期:2011年46-10]
- This paper describes the synthesis and characterization of four new ruthenium complexes containing 1,4 bis(diphenylphosphino)butane (dppb), 2-pyridinecarboxylic acid anion (pic) and the diimines [(2,2'-bipyridine (bipy),...
- Optically active 1,3,4,4-tetrasubstituted beta-lactams: Synthesis and evaluation as tumor cell growth inhibitors
[作者:Perez-Faginas, P; Aranda, MT; Garcia-Lopez, MT; Francesch, A; Cuevas, C; Gonzalez-Muniz, R,期刊:European Journal of Medicinal Chemistry, 页码:5108-5119 , 文章类型: Article,,卷期:2011年46-10]
- The in vitro cytotoxicity assays of several enantiopure (3S,4S)- and (3R,4R)-1,3,4,4-tetrasubstituted beta-lactams derived from amino acids have shown that the (3S,4S)-4-benzyl-1-p-methoxybenzyl-3-methyl-4-methoxycarbony...
- Anticancer and radio-sensitizing evaluation of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety
[作者:Ghorab, MM; Ragab, FA; Heiba, HI; El-Hazek, RM,期刊:European Journal of Medicinal Chemistry, 页码:5120-5126 , 文章类型: Article,,卷期:2011年46-10]
- Recently, it has been reported that compounds bearing a sulfonamide moiety posses many types of biological activities, including anticancer activity. There are a variety of mechanisms for their anticancer activity, and t...
- Synthesis and biological evaluation of 1,9-disubstituted beta-carbolines as potent DNA intercalating and cytotoxic agents
[作者:Chen, ZY; Cao, RH; Shi, BX; Guo, L; Sun, J; Ma, Q; Fan, WX; Song, HC,期刊:European Journal of Medicinal Chemistry, 页码:5127-5137 , 文章类型: Article,,卷期:2011年46-10]
- A series of novel 1,9-disubstituted beta-carbolines was designed, synthesized and evaluated as cytotoxic and DNA intercalating agents. Compounds 7b, 7c, 8b and 8c exhibited the most potent cytotoxic activities with IC(50...
- Synthesis and SAR optimization of diketo acid pharmacophore for HCV NS5B polymerase inhibition
[作者:Bhatt, A; Gurukumar, KR; Basu, A; Patel, MR; Kaushik-Basu, N; Talele, TT,期刊:European Journal of Medicinal Chemistry, 页码:5138-5145 , 文章类型: Article,,卷期:2011年46-10]
- Hepatitis C virus (HCV) NS5B polymerase is a key target for anti-HCV therapeutics development. Here we report the synthesis and biological evaluation of a new series of alpha,gamma-diketo acids (DKAs) as NS5B polymerase ...
- Synthesis, antiproliferative activity and DNA binding study of mixed ammine/cyclohexylamine platinum(II) complexes with 1-(substituted benzyl) azetidine-3, 3-dicarboxylates
[作者:Sun, YY; Gou, SH; Yin, RT; Jiang, PY,期刊:European Journal of Medicinal Chemistry, 页码:5146-5153 , 文章类型: Article,,卷期:2011年46-10]
- A novel series of ammine/cyclohexylamine platinum(II) complexes with 1-(substituted benzyl) azetidine-3, 3-dicarboxylates as leaving groups have been synthesized and characterized. All complexes were characterized by ele...
- Synthesis and pharmacological evaluation of indole-based sigma receptor ligands
[作者:Mesangeau, C; Amata, E; Alsharif, W; Seminerio, MJ; Robson, MJ; Matsumoto, RR; Poupaert, JH; McCurdy, CR,期刊:European Journal of Medicinal Chemistry, 页码:5154-5161 , 文章类型: Article,,卷期:2011年46-10]
- A series of novel indole-based analogs were prepared and their affinities for sigma receptors were determined using in vitro radioligand binding assays. The results of this study identified several compounds with nanomol...
- Synthesis, fluorescence and biodistribution of a bone-targeted near-infrared conjugate
[作者:Mizrahi, DM; Ziv-Polat, O; Perlstein, B; Gluz, E; Margel, S,期刊:European Journal of Medicinal Chemistry, 页码:5175-5183 , 文章类型: Article,,卷期:2011年46-10]
- Enhanced imaging of early-stage bone abnormalities, such as primary tumors or metastases is highly required as the widely-used bone scan frequently lacks the desired sensitivity. Near IR (NIR) fluorescence imaging afford...
- Synthesis and biological activity of novel tiliroside derivants
[作者:Qin, N; Li, CB; Jin, MN; Shi, LH; Duan, HQ; Niu, WY,期刊:European Journal of Medicinal Chemistry, 页码:5189-5195 , 文章类型: Article,,卷期:2011年46-10]
- A series of new tiliroside derivatives were synthesized and characterized by analytical (1)H NMR, (13)C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cel...
- Novel C-4 '' modified azithromycin analogs with remarkably enhanced activity against erythromycin-resistant Streptococcus pneumoniae: The synthesis and antimicrobial evaluation
[作者:Ma, XD; Zhang, L; Wang, RM; Cao, JC; Liu, C; Fang, Y; Wang, JD; Ma, ST,期刊:European Journal of Medicinal Chemistry, 页码:5196-5205 , 文章类型: Article,,卷期:2011年46-10]
- Three novel structural series of C-4 '' modified azithromycin analogs with two amide groups, which were connected by different alkyl linkage, were designed, prepared and evaluated for their in vitro antibacterial activit...
- Discovery of a new class of HMG-CoA reductase inhibitor from Polyalthia longifolia as potential lipid lowering agent
[作者:Sashidhara, KV; Singh, SP; Srivastava, A; Puri, A; Chhonker, YS; Bhatta, RS; Shah, P; Siddiqi, MI,期刊:European Journal of Medicinal Chemistry, 页码:5206-5211 , 文章类型: Article,,卷期:2011年46-10]
- Bioassay guided fractionation of the ethanolic extract of Polyalthia longifolia var. pendula, led to the discovery of the clerodane diterpene, 16 alpha-hydroxycleroda-3, 13 (14) Z-dien-15, 16-olide (1), as a new structur...
- Discovery of gemfibrozil analogues that activate PPAR alpha and enhance the expression of gene CPT1A involved in fatty acids catabolism
[作者:De Filippis, B; Giancristofaro, A; Ammazzalorso, A; D'Angelo, A; Fantacuzzi, M; Giampietro, L; Maccallini, C; Petruzzelli, M; Amoroso, R,期刊:European Journal of Medicinal Chemistry, 页码:5218-5224 , 文章类型: Article,,卷期:2011年46-10]
- A new series of gemfibrozil analogues conjugated with alpha-asarone, trans-stilbene, chalcone, and their bioisosteric modifications were synthesized and evaluated to develop PPAR alpha agonists. In this attempt, we have ...
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