- Structure-based design, synthesis and biological evaluation of N-pyrazole, N '-thiazole urea inhibitors of MAP kinase p38 alpha
[作者:Getlik, M; Grutter, C; Simard, JR; Nguyen, HD; Robubi, A; Aust, B; van Otterlo, WAL; Rauh, D,期刊:European Journal of Medicinal Chemistry, 页码:1-15 , 文章类型: Article,,卷期:2012年48-1]
- In this paper, we present the structure-based design, synthesis and biological activity of N-pyrazole, N'thiazole-ureas as potent inhibitors of p38 alpha mitogen-activated protein kinase (p38 alpha MAPK). Guided by compl...
- Synthesis, antimicrobial, anticancer evaluation and QSAR studies of 6-methyl-4[1-(2-substituted-phenylamino-acetyl)-1H-indol-3-yl]-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl esters
[作者:Sharma, SK; Kumar, P; Narasimhan, B; Ramasamy, K; Mani, V; Mishra, RK; Majeed, AA,期刊:European Journal of Medicinal Chemistry, 页码:16-25 , 文章类型: Article,,卷期:2012年48-1]
- A series of 6-methyl-4-[1-(2-substituted-phenylamino-acetyl)-1H-indol-3-yl]-2-oxo/thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid ethyl esters (1-16) were synthesized and evaluated in vitro for their antimicrobial ...
- Synthesis, structural characterization and in vitro biological screening of some homoleptic copper(II) complexes with substituted guanidines
[作者:Murtaza, G; Rauf, MK; Badshah, A; Ebihara, M; Said, M; Gielen, M; de Vos, D; Dilshad, E; Mirza, B,期刊:European Journal of Medicinal Chemistry, 页码:26-35 , 文章类型: Article,,卷期:2012年48-1]
- A series of homoleptic copper(II) complexes (1a-8a) with N,N',N"-trisubstituted guanidines, [Cu(II) {PhCONHC(NHR)NPh}(2)] (where R = phenyl (1a), n-butyl (2a), sec-butyl (3a), cyclohexyl (4a), 1-naphthyl (5a), 2,4-dichlo...
- Structure-activity relationship of salicylic acid derivatives on inhibition of TNF-alpha dependent NF kappa B activity: Implication on anti-inflammatory effect of N-(5-chlorosalicyloyl)phenethylamine against experimental colitis
[作者:Kim, J; Kang, S; Hong, S; Yum, S; Kim, YM; Jung, Y,期刊:European Journal of Medicinal Chemistry, 页码:36-44 , 文章类型: Article,,卷期:2012年48-1]
- To develop a more potent NF kappa B inhibitor from salicylic acid which is known to inhibit activity of NF kappa B, a transcription factor regulating genes involved in immunity, inflammation and tumorigenesis, derivative...
- Synthesis and in vitro antimycobacterial activity of compounds derived from (R)- and (S)-2-amino-1-butanol - The crucial role of the configuration
[作者:Dobrikov, GM; Valcheva, V; Stoilova-Disheva, M; Momekov, G; Tzvetkova, P; Chimov, A; Dimitrov, V,期刊:European Journal of Medicinal Chemistry, 页码:45-56 , 文章类型: Article,,卷期:2012年48-1]
- The synthesis of 47 structurally diverse compounds incorporating the (R)-2-amino-1-butanol motif has been realized. Ten of these compounds were found to exhibit in vitro specific activity against Mycobacterium tuberculos...
- Straightforward palladium-mediated synthesis and biological evaluation of benzo [j]phenanthridine-7,12-diones as anti-tuberculosis agents
[作者:Cappoen, D; Jacobs, J; Van, TN; Claessens, S; Diels, G; Anthonissen, R; Einarsdottir, T; Fauville, M; Verschaeve, L; Huygen, K; De Kimpe, N,期刊:European Journal of Medicinal Chemistry, 页码:57-68 , 文章类型: Article,,卷期:2012年48-1]
- In 1991, WHO recognized the resurgence of tuberculosis as a global health problem. Although modern chemotherapy is effective against the causative pathogen Mycobacterium tuberculosis, the current drug regimens have faile...
- Synthesis of novel 2, 5-dihydrofuran derivatives and evaluation of their anticancer activity
[作者:Zhang, YK; Zhong, HY; Wang, TT; Geng, DP; Zhang, MF; Li, K,期刊:European Journal of Medicinal Chemistry, 页码:69-80 , 文章类型: Article,,卷期:2012年48-1]
- According to metal-catalyzed [3 + 2] cycloaddition reaction, we synthesized a series of novel 2, 5-dihydrofuran derivatives and evaluated their in vitro anti-cancer activities via MTT method. The bioassay showed that the...
- Synthesis and evaluation of hexahydropyrrolo[3,4-d]isoxazole-4,6-diones as anti-stress agents
[作者:Badru, R; Anand, P; Singh, B,期刊:European Journal of Medicinal Chemistry, 页码:81-91 , 文章类型: Article,,卷期:2012年48-1]
- A series of 2,3-diphenyl-5-(naphthalen-1-yl)-4H-2,3,3a,5,6,6a-hexahydropyrrolo[3,4-d]isoxazole-4,6-dione derivatives were synthesized via 1,3-dipolar cycloaddition of azomethine N-oxides with N-(alpha-naphthyl)maleimide....
- Synthesis of pyrazolo[3,4-b]pyridines under microwave irradiation in multi-component reactions and their antitumor and antimicrobial activities - Part 1
[作者:El-borai, MA; Rizk, HF; Abd-Aal, MF; El-Deeb, IY,期刊:European Journal of Medicinal Chemistry, 页码:92-96 , 文章类型: Article,,卷期:2012年48-1]
- An efficient one-pot synthesis in multi-component system (MRCs) for the preparation of pyrazolo[3,4-b] pyridine derivatives from the reaction of 5-amino-1-phenyl-3-(pyridin-3-yl)-1H-pyrazole with 4-anisaldehyde and p-sub...
- Analogues of doxanthrine reveal differences between the dopamine D(1) receptor binding properties of chromanoisoquinolines and hexahydrobenzo[a] phenanthridines
[作者:Cueva, JP; Chemel, BR; Juncosa, JI; Lill, MA; Watts, VJ; Nichols, DE,期刊:European Journal of Medicinal Chemistry, 页码:97-107 , 文章类型: Article,,卷期:2012年48-1]
- Efforts to develop selective agonists for dopamine D(1)-like receptors led to the discovery of dihydrexidine and doxanthrine, two bioisosteric [beta-phenyldopamine-type full agonist ligands that display selectivity and p...
- Synthesis and biological evaluation of novel indolocarbazoles with anti-angiogenic activity
[作者:Acero, N; Brana, MF; Anorbe, L; Dominguez, G; Munoz-Mingarro, D; Mitjans, F; Piulats, J,期刊:European Journal of Medicinal Chemistry, 页码:108-113 , 文章类型: Article,,卷期:2012年48-1]
- A novel series of indolocarbazoles were synthesized and their antiproliferative activity against HUVEC, LoVo, DLD-1 and ST-486 cell lines, was investigated. Those staurosporine analogs in which a substituted dimethylamin...
- Design, synthesis and biological evaluation of new naphtalene diimides bearing isothiocyanate functionality
[作者:Minarini, A; Milelli, A; Tumiatti, V; Ferruzzi, L; Marton, MR; Turrini, E; Hrelia, P; Fimognari, C,期刊:European Journal of Medicinal Chemistry, 页码:124-131 , 文章类型: Article,,卷期:2012年48-1]
- The synthesis and the biological activities of new derivatives 1-3, characterized by the isothiocyanate (ITC) functionalities coming from sulforaphane (SFN), a well-known anticancer natural product, were reported. The mo...
- Cobalt(II) complexes with non-steroidal anti-inflammatory drug tolfenamic acid: Structure and biological evaluation
[作者:Tsiliou, S; Kefala, LA; Perdih, F; Turel, I; Kessissoglou, DP; Psomas, G,期刊:European Journal of Medicinal Chemistry, 页码:132-142 , 文章类型: Article,,卷期:2012年48-1]
- Cobalt(II) complexes with the non-steroidal anti-inflammatory drug tolfenamic acid in the presence or absence of nitrogen-donor heterocyclic ligands (2,2'-bipyridine, 1,10-phenanthroline, 2,2'-bipyridylamine or pyridine)...
- Synthesis and biological activity of novel organoselenium derivatives targeting multiple kinases and capable of inhibiting cancer progression to metastases
[作者:Bijian, K; Zhang, ZW; Xu, B; Jie, S; Chen, B; Wan, SB; Wu, JH; Jiang, T; Alaoui-Jamali, MA,期刊:European Journal of Medicinal Chemistry, 页码:143-152 , 文章类型: Article,,卷期:2012年48-1]
- The present study reports synthesis and biological activity of novel benzoisoselenazolone compounds derived from ebselen and conjugated to a sugar molecule. Cell proliferation assay using cancer cells combined with in vi...
- Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E(2) synthase-1
[作者:Wiegard, A; Hanekamp, W; Griessbach, K; Fabian, J; Lehr, M,期刊:European Journal of Medicinal Chemistry, 页码:153-163 , 文章类型: Article,,卷期:2012年48-1]
- Microsomal prostaglandin E(2) synthase-1 (mPGES-1) is an enzyme, which is induced during the inflammatory response. Therefore, inhibitors of this enzyme are considered to be potential anti-inflammatory drugs. We have ide...
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