- Design, synthesis and in vitro evaluation of bridgehead fluoromethyl analogs of N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl) cyclohexanecarboxamide (WAY-100635) for the 5-HT(1A) receptor
[作者:Al Hussainy, R; Verbeek, J; van der Born, D; Booij, J; Herscheid, JDM,期刊:European Journal of Medicinal Chemistry, 页码:5728-5735 , 文章类型: Article,,卷期:2011年46-12]
- Fluorinated analogs that are related to the 5-hydroxytryptamine (5-HT(1A)) antagonist, N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxamide (WAY-100635), have been synthesized and their b...
- Discovery of novel anti-inflammatory drug-like compounds by aligning in silico and in vivo screening: The nitroindazolinone chemotype
[作者:Marrero-Ponce, Y; Siverio-Mota, D; Galvez-Llompart, M; Recio, MC; Giner, RM; Garcia-Domenech, R; Torrens, F; Aran, VJ; Cordero-Maldonado, ML; Esguera, CV; de Witte, PAM; Crawford, AD,期刊:European Journal of Medicinal Chemistry, 页码:5736-5753 , 文章类型: Article,,卷期:2011年46-12]
- In this report, we propose the combination of computational methods and in vivo primary screening in zebrafish larvae and confirmatory in mice models as a novel strategy to accelerate anti-inflammatory drug discovery. In...
- New diarylureas and diarylamides containing 1,3,4-triarylpyrazole scaffold: Synthesis, antiproliferative evaluation against melanoma cell lines, ERK kinase inhibition, and molecular docking studies
[作者:Choi, WK; El-Gamal, MI; Choi, HS; Baek, D; Oh, CH,期刊:European Journal of Medicinal Chemistry, 页码:5754-5762 , 文章类型: Article,,卷期:2011年46-12]
- Synthesis of a new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold is described. Their in vitro antiproliferative activities against 9 human melanoma cell lines were tested. Compounds 12,...
- Synthesis and biological evaluation of some new 2-pyrazolines bearing benzene sulfonamide moiety as potential anti-inflammatory and anti-cancer agents
[作者:Bano, S; Javed, K; Ahmad, S; Rathish, IG; Singh, S; Alam, MS,期刊:European Journal of Medicinal Chemistry, 页码:5763-5768 , 文章类型: Article,,卷期:2011年46-12]
- Eight novel 2-pyrazolines (2a-h) were synthesized by the reaction of appropriate chalcones/flavanones with 4-hydrazinonbenzenesulfonamide hydrochloride and tested for anti-inflammatory and anti-cancer activities. Two com...
- New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies
[作者:Park, JH; El-Gamal, MI; Lee, YS; Oh, CH,期刊:European Journal of Medicinal Chemistry, 页码:5769-5777 , 文章类型: Article,,卷期:2011年46-12]
- A series of 18 new imidazo[2,1-b]thiazole derivatives was synthesized. Their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 15, 16, 18, 22, ...
- Anti-tumoral activities of dioncoquinones B and C and related naphthoquinones gained from total synthesis or isolation from plants
[作者:Bringmann, G; Zhang, GL; Hager, A; Moos, M; Irmer, A; Bargou, R; Chatterjee, M,期刊:European Journal of Medicinal Chemistry, 页码:5778-5789 , 文章类型: Article,,卷期:2011年46-12]
- Dioncoquinones belong to a family of natural naphthoquinone products of interest due to their promising anti-tumoral and anti-infective activities. In particular, dioncoquinones A (5) and B (6) have been shown to be high...
- New spirocyclic Delta(2)-isoxazoline derivatives related to selective agonists of alpha 7 neuronal nicotinic acetylcholine receptors
[作者:Dallanoce, C; Frigerio, F; Grazioso, G; Matera, C; Visconti, GL; De Amici, M; Pucci, L; Pistillo, F; Fucile, S; Gotti, C; Clementi, F; De Micheli, C,期刊:European Journal of Medicinal Chemistry, 页码:5790-5799 , 文章类型: Article,,卷期:2011年46-12]
- A set of structural analogues of spirocyclic quinuclidinyl-Delta(2)-isoxazolines, characterized as potent and selective alpha 7 nicotinic agonists, was prepared and assayed for binding affinity at alpha 7 and alpha 4 bet...
- Anti-hepatocellular carcinoma activity using human HepG2 cells and hepatotoxicity of 6-substituted methyl 3-aminothieno[3,2-b]pyridine-2-carboxylate derivatives: In vitro evaluation, cell cycle analysis and QSAR studies
[作者:Abreu, RMV; Ferreira, ICFR; Calhelha, RC; Lima, RT; Vasconcelos, MH; Adega, F; Chaves, R; Queiroz, MJRP,期刊:European Journal of Medicinal Chemistry, 页码:5800-5806 , 文章类型: Article,,卷期:2011年46-12]
- Hepatocellular carcinoma (HCC) is a highly complex cancer, resistant to commonly used treatments and new therapeutic agents are urgently needed. A total of thirty-two thieno[3,2-b]pyridine derivatives of two series: meth...
- Amine-alkyl derivatives of hydantoin: New tool to combat resistant bacteria
[作者:Handzlik, J; Szymanska, E; Chevalier, J; Otrgbska, E; Kiec-Kononowicz, K; Pages, JM; Alibert, S,期刊:European Journal of Medicinal Chemistry, 页码:5807-5816 , 文章类型: Article,,卷期:2011年46-12]
- A series of new 5,5-diphenylhydantoin derivatives with various amine alkyl terminal fragments at N1-position were synthesized. Then a series of twenty-eight compounds with the same hydantoin scaffold were evaluated for t...
- Synthesis and apoptosis inducing ability of new anilino substituted pyrimidine sulfonamides as potential anticancer agents
[作者:Kamal, A; Dastagiri, D; Ramaiah, MJ; Reddy, JS; Bharathi, EV; Reddy, MK; Sagar, MVP; Reddy, TL; Pushpavalli, SNCVL; Pal-Bhadra, M,期刊:European Journal of Medicinal Chemistry, 页码:5817-5824 , 文章类型: Article,,卷期:2011年46-12]
- A series of anilino substituted pyrimidine sulfonamides were prepared and evaluated for their anticancer activity. These sulfonamides showed promising activity with IC(50) values ranging from 5.6 to 12.3 mu M. The detail...
- Design, synthesis and biological study of novel pyrido[2,3-d]pyrimidine as anti-proliferative CDK2 inhibitors
[作者:Ibrahim, DA; Ismail, NSM,期刊:European Journal of Medicinal Chemistry, 页码:5825-5832 , 文章类型: Article,,卷期:2011年46-12]
- The design and synthesis of a small library of 4-aminopyrido[2,3-d]pyrimidine derivatives is reported. The potential activity of these compounds as CDK2/Cyclin A, CDK4/Cyclin D, EGFR and anti-tumor was evaluated by cytot...
- 2D MI-DRAGON: A new predictor for protein-ligands interactions and theoretic-experimental studies of US FDA drug-target network, oxoisoaporphine inhibitors for MAO-A and human parasite proteins
[作者:Prado-Prado, F; Garcia-Mera, X; Escobar, M; Sobarzo-Sanchez, E; Yanez, M; Riera-Fernandez, P; Gonzalez-Diaz, H,期刊:European Journal of Medicinal Chemistry, 页码:5838-5851 , 文章类型: Article,,卷期:2011年46-12]
- There are many pairs of possible Drug-Proteins Interactions that may take place or not (DPIs/nDPIs) between drugs with high affinity/non-affinity for different proteins. This fact makes expensive in terms of time and res...
- Molecular modeling study and synthesis of novel dicationic flexible triaryl guanidines and imidamides as antiprotozoal agents
[作者:Arafa, RK; Wenzler, T; Brun, R; Chai, Y; Wilson, WD,期刊:European Journal of Medicinal Chemistry, 页码:5852-5860 , 文章类型: Article,,卷期:2011年46-12]
- A new series of fourteen dicationic flexible triaryl bis-guanidines 3a,b, bis-N-substituted guanidines 7a,b and 8a,b as well as bis-imidamides 9-12a,b having a 1,3- or 1,4-diphenoxybenzene scaffold backbone were synthesi...
- Synthesis and biological evaluation of novel nitrogen- and sulfur-containing hetero-1,4-naphthoquinones as potent antifungal and antibacterial agents
[作者:Ibis, C; Tuyun, AF; Ozsoy-Gunes, Z; Bahar, H; Stasevych, MV; Musyanovych, RY; Komarovska-Porokhnyavets, O; Novikov, V,期刊:European Journal of Medicinal Chemistry, 页码:5861-5867 , 文章类型: Article,,卷期:2011年46-12]
- 1,4-Naphthoquinones are unique reagents in organic synthesis and have been employed in several well known and recently developed areas of application. Furthermore, these 1,4-naphthoquinones have demonstrated high reactiv...
- Synthesis and cytotoxic activity of novel 3-(1H-indol-3-yl)-1H-pyrazole-5-carbohydrazide derivatives
[作者:Zhang, DT; Wang, GT; Zhao, GL; Xu, WR; Huo, LY,期刊:European Journal of Medicinal Chemistry, 页码:5868-5877 , 文章类型: Article,,卷期:2011年46-12]
- A series of novel 3-(1H-indole-3-yl)-1H-pyrazole-5-carbohydrazide derivatives 4Ia-n, 4IIa-b and 6 were prepared by hydrazinolysis of ethyl 3-(1H-indole-3-yl)-1H-pyrazole-5-carboxylate with hydrazine hydrate in excellent ...
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