- Bromoalkoxyxanthones as promising antitumor agents: Synthesis, crystal structure and effect on human tumor cell lines
[作者:Sousa, E; Paiva, A; Nazareth, N; Gales, L; Damas, AM; Nascimento, MSJ; Pinto, M,期刊:European Journal of Medicinal Chemistry, 页码:3830-3835 , 文章类型: Article,,卷期:2009年44-9]
In a study involving the synthesis of bis-intercalators, a bisxanthone and a minor product, 1-(6-bromohexyloxy)-xanthone were obtained. Although no capacity to inhibit the growth of human tumor cell lines was observed...
- New imidazo[1,2-a]quinoxaline derivatives: Synthesis and in vitro activity against human melanoma
[作者:Deleuze-Masquefa, C; Moarbess, G; Khier, S; David, N; Gayraud-Paniagua, S; Bressolle, F; Pinguet, F; Bonnet, PA,期刊:European Journal of Medicinal Chemistry, 页码:3406-3411 , 文章类型: Article,,卷期:2009年44-9]
- New imidazo[1,2-a] quinoxaline analogues have been synthesized in good yields via a bimolecular condensation of 2-imidazole carboxylic acid, followed by a coupling with ortho-fluoroaniline and subsequent substitution on ...
- Bibenzyl- and stilbene-core compounds with non-polar linker atom substituents as selective ligands for estrogen receptor beta
[作者:Waibel, M; De Angelis, M; Stossi, F; Kieser, KJ; Carlson, KE; Katzenellenbogen, BS; Katzenellenbogen, JA,期刊:European Journal of Medicinal Chemistry, 页码:3412-3424 , 文章类型: Article,,卷期:2009年44-9]
- A series of structurally simple bibenzyl-diol and stilbene-diol core molecules, structural analogs of the well-known hexestrol and diethylstilbestrol non-steroidal estrogens, were prepared and evaluated as estrogen recep...
- 2D-and 3D-QSAR studies on 54 anti-tumor Rubiaceae-type cyclopeptides
[作者:Yan, H; Pan, XL; Tan, NH; Fan, JT; Zeng, GZ; Han, HJ,期刊:European Journal of Medicinal Chemistry, 页码:3425-3432 , 文章类型: Article,,卷期:2009年44-9]
RA-VII, a bicyclic hexapeptide isolated from the roots of Rubia cordifolia, Rubia akane belongs to Rubiaceae-type cyclopeptides (RAS) and has attracted much attention for its potent anti-tumor activity and its bicycli...
- Novel topoisomerase I-targeting antitumor agents synthesized from the N,N,N-trimethylammonium derivative of ARC-111, 5H-2,3-dimethoxy-8,9-methylenedioxy-5-[(2-N,N,N-trimethylammonium)ethyl]dibenzo[c,h][1,6]naphthyridin-6-one iodide
[作者:Feng, W; Satyanarayana, M; Tsai, YC; Liu, AA; Liu, LF; LaVoie, EJ,期刊:European Journal of Medicinal Chemistry, 页码:3433-3438 , 文章类型: Article,,卷期:2009年44-9]
- Several new TOP1-targeting agents were prepared using as an intermediate the N,N,N-trimethyl quaternary ammonium salt 2 of ARC-111. Direct displacement of the quaternary ammonium group with hydroxide, cyclopropylamine, i...
- CoMFA, LeapFrog and blind docking studies on sulfonanilide derivatives acting as selective aromatase expression regulators
[作者:Gueto, C; Torres, J; Vivas-Reyes, R,期刊:European Journal of Medicinal Chemistry, 页码:3445-3451 , 文章类型: Article,,卷期:2009年44-9]
- Aromatase, the enzyme responsible for estrogen biosynthesis, is an attractive target in the treatment of hormone-dependent breast cancer. In this manuscript, the structure-based drug design approach of sulfonanilide anal...
- Palladium(II) complexes with R(2)edda-derived ligands. Part II. Synthesis, characterization and in vitro antitumoral studies of R(2)eddip esters and palladium(II) complexes
[作者:Zmejkovski, BB; Kaluderovic, GN; Gomez-Ruiz, S; Zizak, Z; Steinborn, D; Schmidt, H; Paschke, R; Juranic, ZD; Sabo, TJ,期刊:European Journal of Medicinal Chemistry, 页码:3452-3458 , 文章类型: Article,,卷期:2009年44-9]
- New R(2)eddip-type esters (R = cyclopentyl, L3 center dot 2HCl 1.5H(2)O; cyclohexyl, L4 center dot 2HCl center dot H2O) and corresponding palladium(II) complexes, [PdCl(2)L3] (3) and [PdCl2L4]center dot H2O (4), as well ...
- Novel ureas and thioureas of 15-membered azalides with antibacterial activity against key respiratory pathogens
[作者:Krajacic, MB; Novak, P; Dumic, M; Cindric, M; Paljetak, HC; Kujundzic, N,期刊:European Journal of Medicinal Chemistry, 页码:3459-3470 , 文章类型: Article,,卷期:2009年44-9]
- The new ureas and thioureas of 15-membered azalides, N ''-substituted 9a-(N'-carbamoyl-gamma-aminopropyl) (4), 9a-(N'-thiocarbamoyl-gamma-aminopropyl) (6), 9a-[N'-(beta-cyanoethyl)-N'-(carbamoyl-gamma-aminopropyl)] (8) a...
- 5-Benzylidene-hydantoins: Synthesis and antiproliferative activity on A549 lung cancer cell line
[作者:Zuliani, V; Carmi, C; Rivara, M; Fantini, M; Lodola, A; Vacondio, F; Bordi, F; Plazzi, PV; Cavazzoni, A; Galetti, M; Alfieri, RR; Petronini, PG; Mora, M,期刊:European Journal of Medicinal Chemistry, 页码:3471-3479 , 文章类型: Article,,卷期:2009年44-9]
- Benzylidene hydantoins have been recently reported as a new class of EGFR inhibitors. We describe here a simple and efficient methodology for the parallel solution-phase synthesis of a library of 5-benzylidene hydantoins...
- Physicochemical properties and membrane interactions of anti-apoptotic derivatives 2-(4-fluorophenyl)-3-(pyridin-4-yl)imidazo[1,2-a]pyridine depending on the hydroxyalkylamino side chain length and conformation: An NMR and ESR study
[作者:Follot, S; Debouzy, JC; Crouzier, D; Enguehard-Gueiffier, C; Gueiffier, A; Nachon, F; Lefebvre, B; Fauvelle, F,期刊:European Journal of Medicinal Chemistry, 页码:3509-3518 , 文章类型: Article,,卷期:2009年44-9]
- Three imidazo[1,2-a]pyridine derivatives 3a-c have been synthesized from p38 kinase inhibitor structures and evaluated as anti-apoptosis agents. These drugs were designed to interact with nucleic acids and membrane inter...
- Synthesis and cytotoxic activity of alpha-santonin derivatives
[作者:Arantes, FFP; Barbosa, LCA; Alvarenga, ES; Demuner, AJ; Bezerra, DP; Ferreira, JRO; Costa-Lotufo, LV; Pessoa, C; Moraes, MO,期刊:European Journal of Medicinal Chemistry, 页码:3739-3745 , 文章类型: Article,,卷期:2009年44-9]
- Ten alpha-santonin derivatives were synthesized in moderate to high yields. Four derivatives namely 10 alpha-acetoxy-3-oxo-1,7 alpha H,6,11 beta H-guai-4-en-6,12-olide (2), isofotosantonic acid (3), 10 alpha-hydroxy-3-ox...
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