- Selective and potent agonists for estrogen receptor beta derived from molecular refinements of salicylaldoximes
[作者:Bertini, S; De Cupertinis, A; Granchi, C; Bargagli, B; Tuccinardi, T; Martinelli, A; Macchia, M; Gunther, JR; Carlson, KE; Katzenellenbogen, JA; Minutolo, F,期刊:European Journal of Medicinal Chemistry, 页码:2453-2462 , 文章类型: Article,,卷期:2011年46-6]
- In a continuing effort to improve the subtype selectivity and agonist potency of estrogen receptor beta (ER beta) ligands, we have designed and developed a thus far unexplored structural series obtained by molecular refi...
- Potential virtual lead identification in the discovery of renin inhibitors: Application of ligand and structure-based pharmacophore modeling approaches
[作者:Thangapandian, S; John, S; Sakkiah, S; Lee, KW,期刊:European Journal of Medicinal Chemistry, 页码:2469-2476 , 文章类型: Article,,卷期:2011年46-6]
- Renin, an enzyme by cleaving angiotensinogen to angiotensin-I, controls the first and rate-limiting step of renin-angiotensin system that is associated with blood pressure. Thus Ligand and structure-based pharmacophore m...
- Discovery of polyoxometalate-based HDAC inhibitors with profound anticancer activity in vitro and in vivo
[作者:Dong, ZX; Tan, RK; Cao, J; Yang, Y; Kong, CF; Du, J; Zhu, S; Zhang, Y; Lu, J; Huang, BQ; Liu, SX,期刊:European Journal of Medicinal Chemistry, 页码:2477-2484 , 文章类型: Article,,卷期:2011年46-6]
- We obtained 5 positive novel histone deacetylase inhibitors (HDACIs) from a polyoxometalate (POM) library by using a cell-based screening system targeting the p21 gene promoter. Among them, PAC-320, a new tri-organic-tin...
- Synthesis and antiproliferative evaluation of 23-hydroxybetulinic acid derivatives
[作者:Lan, P; Wang, J; Zhang, DM; Shu, C; Cao, HH; Sun, PH; Wu, XM; Ye, WC; Chen, WM,期刊:European Journal of Medicinal Chemistry, 页码:2490-2502 , 文章类型: Article,,卷期:2011年46-6]
- Based on structural modifications of the natural 23-hydroxybetulinic acid, a series of novel its derivatives had been synthesized. The new compounds were screened for in vitro antiproliferative activity against cancer ce...
- New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents
[作者:Thomas, KD; Adhikari, AV; Chowdhury, IH; Sumesh, E; Pal, NK,期刊:European Journal of Medicinal Chemistry, 页码:2503-2512 , 文章类型: Article,,卷期:2011年46-6]
- Three new series of quinoline-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines were synthesized through multi-step reactions. The required intermediate, [1-(6-methoxy-2-methylquinolin-4-yl)-1H-1,2...
- Discovery of new nanomolar peroxisome proliferator-activated receptor gamma activators via elaborate ligand-based modeling
[作者:Al-Najjar, BO; Wahab, HA; Muhammad, TST; Shu-Chien, AC; Noruddin, NAA; Taha, MO,期刊:European Journal of Medicinal Chemistry, 页码:2513-2529 , 文章类型: Article,,卷期:2011年46-6]
- Peroxisome Proliferator-Activated Receptor gamma (PPAR gamma) activators have drawn great recent attention in the clinical management of type 2 diabetes mellitus, prompting several attempts to discover and optimize new P...
- Synthesis, characterization, and study on HeLa cells activity of a dinuclear complex [Cu(4)(phen)(4)(H(2)O)(2)]center dot(pyri)center dot 3H(2)O
[作者:Gao, EJ; Lin, L; Zhang, Y; Wang, RS; Zhu, MC; Liu, SH; Sun, TD; Jiao, W; Andrey, VZ,期刊:European Journal of Medicinal Chemistry, 页码:2546-2554 , 文章类型: Article,,卷期:2011年46-6]
- The complex [Cu(4)(phen)(4)(H(2)O)(2)]center dot(pyri)center dot 3H(2)O(where phen = 1,10-phenanthroline and pyri = 3,5-pyridine dicarboxylic acid)has been synthesized and characterized. IR spectra, elemental analysis an...
- Synthesis and antimicrobial activity of some new 4-hetarylpyrazole and furo[2,3-c]pyrazole derivatives
[作者:Bondock, S; Khalifa, W; Fadda, AA,期刊:European Journal of Medicinal Chemistry, 页码:2555-2561 , 文章类型: Article,,卷期:2011年46-6]
- In continuation of our efforts to find a new class of antimicrobial agents, a series of 4-hetarylpyrazoles and furo[2,3-c]pyrazoles were prepared via the reaction of 2-chloro-1-(5-hydroxy-3-methyl-1-phenyl-1H-pyrazol-4-y...
- Prenylated derivatives of baicalein and 3,7-dihydroxyflavone: Synthesis and study of their effects on tumor cell lines growth, cell cycle and apoptosis
[作者:Neves, MP; Cidade, H; Pinto, M; Silva, AMS; Gales, L; Damas, AM; Lima, RT; Vasconcelos, MH; Nascimento, MDJ,期刊:European Journal of Medicinal Chemistry, 页码:2562-2574 , 文章类型: Article,,卷期:2011年46-6]
- Fourteen baicalein and 3,7-dihydroxyflavone derivatives were synthesized and evaluated for their inhibitory activity against the in vitro growth of three human tumor cell lines. The synthetic approaches were based on the...
- Antioxydant activity of beta-carboline derivatives in the LDL oxidation model
[作者:Hadjaz, F; Besret, S; Martin-Nizard, F; Yous, S; Dilly, S; Lebegue, N; Chavatte, P; Duriez, P; Berthelot, P; Carato, P,期刊:European Journal of Medicinal Chemistry, 页码:2575-2585 , 文章类型: Article,,卷期:2011年46-6]
- A series of beta-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO...
- Anticancer effects of the metabolic products of the resveratrol analogue, DMU-212: Structural requirements for potency
[作者:Androutsopoulos, VP; Ruparelia, KC; Papakyriakou, A; Filippakis, H; Tsatsakis, AM; Spandidos, DA,期刊:European Journal of Medicinal Chemistry, 页码:2586-2595 , 文章类型: Article,,卷期:2011年46-6]
- The methoxylated trans-stilbene resveratrol analogue, (E)-3,4,5,4'-tetramethoxystilbene (1), has shown promising antiproliferative activity in in vitro cell line and in vivo models. In vivo I gives rise to several metabo...
- Inhibition of alpha-glucosidase and alpha-amylase by diaryl derivatives of imidazole-thione and 1,2,4-triazole-thiol
[作者:Balba, M; Abd El-Hady, N; Taha, N; Rezki, N; El Ashry, EH,期刊:European Journal of Medicinal Chemistry, 页码:2596-2601 , 文章类型: Article,,卷期:2011年46-6]
- The in vivo and in vitro effects of 4,5-diphenylimidazole-2-thione (1), 4,5-Diphenyl-1,2,4-triazole-3-thiol (2) and 5-(2-Hydroxyphenyl)-4-phenyl-12,4-triazole-3-thiol (3) on alpha-glucosidase and alpha-amylase were inves...
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