- Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists
[作者:Tomassoli, I; Ismaili, L; Pudlo, M; de los Rios, C; Soriano, E; Colmena, I; Gandia, L; Rivas, L; Samadi, A; Marco-Contelles, J; Refouvelet, B,期刊:European Journal of Medicinal Chemistry, 页码:1-10 , 文章类型: Article,,卷期:2011年46-1]
- The synthesis, biological evaluation, and molecular modeling of new 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides(4), 4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carbohydrazide (6), and some hexahydropyrimido[5,4-c]quin...
- Chiral 1,5-disubstituted 1,3,5-hexahydrotriazine-2-N-nitroimine analogues as novel potent neonicotinoids: Synthesis, insecticidal evaluation and molecular docking studies
[作者:Sun, CW; Zhu, J; Wang, HF; Jin, J; Xing, JH; Yang, DR,期刊:European Journal of Medicinal Chemistry, 页码:11-20 , 文章类型: Article,,卷期:2011年46-1]
- A new series of 1,5-disubstituted 1,3,5-hexahydrotriazine-2-N-nitroimines (4a-4x) were designed and synthesized as novel chiral neonicotinoid analogues. The single-crystal structure of 4n was further determined by X-ray ...
- Synthesis, in vitro antimicrobial and in vivo antitumor evaluation of novel pyrimidoquinolines and its nucleoside derivatives
[作者:Abbas, HAS; Hafez, HN; El-Gazzar, ARBA,期刊:European Journal of Medicinal Chemistry, 页码:21-30 , 文章类型: Article,,卷期:2011年46-1]
- Seven series of pyrimidoquinoline derivatives have been synthesized, tetrazolo[4',3':-1,2]pyrimido[4,5-b] quinoline (3), 2-aminopyrimido[4,5-b]quinoline (4), triazolo[4',3':1,2]-pyrimidoquinoline (5a,b, 10), imidazolo[3'...
- Synthesis and antimycobacterial activity of a series of ferrocenyl derivatives
[作者:Maguene, GM; Jakhlal, J; Ladyman, M; Vallin, A; Ralambomanana, DA; Bousquet, T; Maugein, J; Lebibi, J; Pelinski, L,期刊:European Journal of Medicinal Chemistry, 页码:31-38 , 文章类型: Article,,卷期:2011年46-1]
- In this work we reported the synthesis and evaluation of Mycobacterium tuberculosis activities in vitro of a series of twenty five ferrocenyl derivatives: ferrocenyl amides derived from nicotinamide and pyrazinamide, fer...
- Microwave supported synthesis of some novel 1,3-Diarylpyrazino[1,2-a] benzimidazole derivatives and investigation of their anticancer activities
[作者:Demirayak, S; Kayagil, I; Yurttas, L,期刊:European Journal of Medicinal Chemistry, 页码:411-416 , 文章类型: Article,,卷期:2011年46-1]
- The syntheses of 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and the investigation of their anticancer activities were studied. For this, 2-aryloylbenzimidazole derivatives were reacted with 2-bromoacetophenones i...
- Synthesis and in vitro cytotoxic evaluation of some thiazolylbenzimidazole derivatives
[作者:Luo, Y; Xiao, F; Qian, SJ; Lu, W; Yang, B,期刊:European Journal of Medicinal Chemistry, 页码:417-422 , 文章类型: Article,,卷期:2011年46-1]
- A novel kind of thiazolylbenzimidazole derivatives were designed and synthesized and evaluated for their antitumor activity against SMMC-7721 and A549 cell lines. Most compounds showed good antitumor activities, and comp...
- The first series of 4,11-bis[(2-aminoethyl)amino]anthra[2,3-b]furan-5,10-diones: Synthesis and anti-proliferative characteristics
[作者:Shchekotikhin, AE; Glazunova, VA; Dezhenkova, LG; Shevtsova, EK; Traven', VF; Balzarini, J; Huang, HS; Shtil, AA; Preobrazhenskaya, MN,期刊:European Journal of Medicinal Chemistry, 页码:423-428 , 文章类型: Article,,卷期:2011年46-1]
- We developed the synthesis of a series of furan-fused tetracyclic analogues of the antitumor agent ametantrone. The reactions included nucleophilic substitution of propoxy groups in 4,11-dipropoxyanthra[2,3-b]furan-5,10-...
- Receptor-dependent (RD) 3D-QSAR approach of a series of benzylpiperidine inhibitors of human acetylcholinesterase (HuAChE)
[作者:Araujo, JQ; de Brito, MA; Hoelz, LVB; de Alencastro, RB; Castro, HC; Rodrigues, CR; Albuquerque, MG,期刊:European Journal of Medicinal Chemistry, 页码:39-51 , 文章类型: Article,,卷期:2011年46-1]
- Acetylcholine inhibitors (AChEIs) are currently considered as potential drugs for treating Alzheimer disease. In this work, we developed a receptor-dependent 3D-QSAR (RD-3D-QSAR) models based on a series of 60 benzylpipe...
- Self-organizing molecular field analysis on human beta-secretase nonpeptide inhibitors: 5, 5-disubstituted aminohydantoins
[作者:Li, Z; Zhou, M; Wu, F; Li, R; Ding, ZY,期刊:European Journal of Medicinal Chemistry, 页码:58-64 , 文章类型: Article,,卷期:2011年46-1]
- 5, 5-disubstituted aminohydantoins have been recently reported as potent and selective human beta-secretase (BACE-1) inhibitors. Self-Organizing Molecular Field Analysis (SOMFA) is used to study the correlation between t...
- Discovery of a novel nitroimidazolyl-oxazolidinone hybrid with potent anti Gram-positive activity: Synthesis and antibacterial evaluation
[作者:Khalaj, A; Nakhjiri, M; Negahbani, AS; Samadizadeh, M; Firoozpour, L; Rajabalian, S; Samadi, N; Faramarzi, MA; Adibpour, N; Shafiee, A; Foroumadi, A,期刊:European Journal of Medicinal Chemistry, 页码:65-70 , 文章类型: Article,,卷期:2011年46-1]
- A number of linezolid analogues containing a nitroaryl-1,3,4-thiadiazole moiety, were prepared and evaluated as antibacterial agents against a panel of Gram-positive and Gram-negative bacteria. Among synthesized compound...
- Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(+/-)-MRJF4] in prostate cancer cells
[作者:Marrazzo, A; Fiorito, J; Zappala, L; Prezzavento, O; Ronsisvalle, S; Pasquinucci, L; Scoto, GM; Bernardini, R; Ronsisvalle, G,期刊:European Journal of Medicinal Chemistry, 页码:433-438 , 文章类型: Article,,卷期:2011年46-1]
- Complex mechanisms of prostate cancer progression prompt to novel therapeutic strategies concerning a combination of drugs or of single molecules able to interact with more crucial targets. Histone deacetylase inhibitors...
- Synthesis of a novel ester of hydroxytyrosol and alpha-lipoic acid exhibiting an antiproliferative effect on human colon cancer HT-29 cells
[作者:Bernini, R; Crisante, F; Merendino, N; Molinari, R; Soldatelli, MC; Velotti, F,期刊:European Journal of Medicinal Chemistry, 页码:439-446 , 文章类型: Article,,卷期:2011年46-1]
- A novel ester of hydroxytyrosol and alpha-lipoic acid was synthesized in satisfactory yield by original and simple procedures and evaluated about its antiproliferative activity on the human colorectal adenocarcinoma HT-2...
- The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes
[作者:Deng, JF; Peng, L; Zhang, GC; Lan, XB; Li, CF; Chen, FX; Zhou, YY; Lin, ZX; Chen, L; Dai, RK; Xu, HJ; Yang, L; Zhang, XQ; Hu, WH,期刊:European Journal of Medicinal Chemistry, 页码:71-76 , 文章类型: Article,,卷期:2011年46-1]
- New dipeptidyl peptidase IV inhibitors were designed based on Alogliptin using a scaffold-hopping strategy. All of the compounds constructed on a thienopyrimidine scaffold demonstrated good inhibition and selectivity for...
- Molecular modeling studies on imidazo[4,5-b]pyridine derivatives as Aurora A kinase inhibitors using 3D-QSAR and docking approaches
[作者:Lan, P; Chen, WN; Chen, WM,期刊:European Journal of Medicinal Chemistry, 页码:77-94 , 文章类型: Article,,卷期:2011年46-1]
- 3D-QSAR and docking studies were performed on sixty imidazo[4,5-b]pyridine derivatives as Aurora A kinase inhibitors. The CoMFA and CoMSIA models using forthy-eight molecules in the training set, gave r(cv)(2) values of ...
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