- Synthesis and antiprotozoal activity of 4-arylcoumarins
[作者:Pierson, JT; Dumetre, A; Hutter, S; Delmas, F; Laget, M; Finet, JP; Azas, N; Combes, S,期刊:European Journal of Medicinal Chemistry, 页码:864-869 , 文章类型: Article,,卷期:2010年45-3]
- A large series of 4-arylcoumarins was synthesized by Suzuki-Miyaura cross-coupling reaction and evaluated for antiprotozoal activity against: Plasmodium falciparum and Leishmania donovani. Several compounds were found to...
- Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core
[作者:Wangsell, F; Gustafsson, K; Kvarnstrom, I; Borkakoti, N; Edlund, M; Jansson, K; Lindberg, J; Hallberg, A; Rosenquist, A; Samuelsson, B,期刊:European Journal of Medicinal Chemistry, 页码:870-882 , 文章类型: Article,,卷期:2010年45-3]
- We herein describe the design and synthesis of a series of BACE-1 inhibitors incorporating a P1-substituted hydroxyl ethylene transition state isostere. The synthetic route starting from commercially available carbohydra...
- Synthesis, characterization and biocidal activity of new organotin complexes of 2-(3-oxocyclohex-1-enyl)benzoic acid
[作者:Vieira, FT; de Lima, GM; Maia, JRD; Speziali, NL; Ardisson, JD; Rodrigues, L; Correa, A; Romero, OB,期刊:European Journal of Medicinal Chemistry, 页码:883-889 , 文章类型: Article,,卷期:2010年45-3]
- The reaction of 1,3-cyclohexadione with 2-aminobenzoic acid has produced the 2-(3-oxocyclohex-1-enyl)benzoic acid (HOBz). Subsequent reactions of the ligand with organotin chlorides led to [Me2Sn(OBz)O](2) (1), [Bu2Sn(OB...
- Novel phosphoramidates with porphine and nitrogenous drug: One-pot synthesis and orientation to cancer cells
[作者:Wang, ZW; Guo, CC; Xie, WZ; Liu, CZ; Mao, CG; Tan, Z,期刊:European Journal of Medicinal Chemistry, 页码:890-895 , 文章类型: Article,,卷期:2010年45-3]
- One-pot synthesis of novel phosphoramidates with porphine and nitrogenous drug was accomplished. In the absence of light, MTT test showed that they killed the BEL-7402 liver cancer cells effectively in vitro. The cell vi...
- 5-Substituted [1]pyrindine derivatives with antiproliferative activity
[作者:Kolb, S; Goddard, ML; Loukaci, A; Mondesert, O; Ducommun, B; Braud, E; Garbay, C,期刊:European Journal of Medicinal Chemistry, 页码:896-901 , 文章类型: Article,,卷期:2010年45-3]
- We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a. cervical carcinoma tumor cell line, and on the melanoma A2058 cell line....
- Simultaneous tritium labelling of two potent 5-HT4 ligands
[作者:Sobrio, F; Lemaitre, S; Hinsberger, A; Barre, L; Rousseau, B; Rault, S,期刊:European Journal of Medicinal Chemistry, 页码:1263-1265 , 文章类型: Article,,卷期:2010年45-3]
- Two potent and selective 5-HT4 ligands, [H-3]-5-[(N-propylpiperidin-4-yl)methoxy]-1,2,3,4-tetrahydrobenzo[h][1,6] naphthyricline (1a) and [H-3]-1-methyl-5-[(N-propylpiperidin-4-yl)methoxy]pyrrolo[1,2-a]thieno[2,3-e]pyraz...
- Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives
[作者:Sondhi, SM; Rani, R; Roy, P; Agrawal, SK; Saxena, AK,期刊:European Journal of Medicinal Chemistry, 页码:902-908 , 文章类型: Article,,卷期:2010年45-3]
- Heterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, an...
- Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors
[作者:Sahoo, PK; Behera, P,期刊:European Journal of Medicinal Chemistry, 页码:909-914 , 文章类型: Article,,卷期:2010年45-3]
- The acetic acid derivatives of [1,2,4]triazino[4,3-a]benzimidazole (TBI) were synthesized and tested in vitro and in vivo as selective aldose reductase (ALR2) inhibitors. Compound PS11 showed highest inhibitory activity ...
- Synthesis and antibacterial activity of novel 3-O-carbamoyl derivatives of clarithromycin and 11,12-cyclic carbonate azithromycin
[作者:Zhang, L; Song, LC; Liu, ZP; Li, H; Lu, YD; Li, ZR; Ma, ST,期刊:European Journal of Medicinal Chemistry, 页码:915-922 , 文章类型: Article,,卷期:2010年45-3]
- Two series of novel 3-O-carbamoyl derivatives of clarithromycin and 11,12-cyclic carbonate azithromycin were designed, synthesized and evaluated for their in vitro antibacterial activities. Compounds 4j and 4k were the m...
- Synthesis and biological activity of derivatives of the marine quinone avarone
[作者:Bozic, T; Novakovic, I; Gasic, MJ; Juranic, Z; Stanojkovic, T; Tufegdzic, S; Kljajic, Z; Sladic, D,期刊:European Journal of Medicinal Chemistry, 页码:923-929 , 文章类型: Article,,卷期:2010年45-3]
- Nine alkyl(aryl)thio derivatives of the marine sesquiterpene quinone avarone were synthesized by nucleophilic addition of thiols or thiophenol to avarone. In most cases only one regioisomer was obtained. Their cytotoxic ...
- Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species
[作者:Changtam, C; de Koning, HP; Ibrahim, H; Sajid, MS; Gould, MK; Suksamrarn, A,期刊:European Journal of Medicinal Chemistry, 页码:941-956 , 文章类型: Article,,卷期:2010年45-3]
- The natural curcuminoids curcumin (1), demethoxycurcumin (2) and bisdemethoxycurcumin (3) have been chemically modified to give 46 analogs and 8 pairs of 1: 1 mixture of curcuminoid analogs and these parent curcuminoids ...
- CoMFA and molecular docking studies of benzoxazoles and benzothiazoles as CYP450 1A1 inhibitors
[作者:Pan, J; Liu, GY; Cheng, J; Chen, XJ; Ju, XL,期刊:European Journal of Medicinal Chemistry, 页码:967-972 , 文章类型: Article,,卷期:2010年45-3]
- For better understanding of the molecular interactions of inhibitors with CYP450 1A1, a series of benzoxazoles and benzothiazoles were analyzed by comparative molecular field analysis (CoMFA) and molecular docking. Two c...
- Synthesis and antitumor activity of new dihydropyridine thioglycosides and their corresponding dehydrogenated forms
[作者:Abbas, HAS; El Sayed, WA; Fathy, NM,期刊:European Journal of Medicinal Chemistry, 页码:973-982 , 文章类型: Article,,卷期:2010年45-3]
- A number of a new pyridine thioglycosides were synthesized via reaction of piperidinium salts of dihydropyridinethiones with 2,3,4,6-tetra-O-acetyl-alpha-D-gluco- and galactopyranosyl bromide. The antitumor activities of...
- Molecular modeling study of binding site selectivity of TQMP to G-quadruplex DNA
[作者:Li, AX; Maurel, F; Barbault, F; Delamar, M; Wang, BS; Zhou, X; Wang, P,期刊:European Journal of Medicinal Chemistry, 页码:983-991 , 文章类型: Article,,卷期:2010年45-3]
- Molecular dynamics (MD) simulations of four-stranded G-quadruplex DNA complexes formed by the sequence d(TTAGGG)(4) and the TQMP ligand are presented. The TQMP complex was examined both in two possible binding modes (dia...
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