- Growth inhibition of Mycobacterium smegmatis by prodrugs of deoxyxylulose phosphate reducto-isomerase inhibitors, promising anti-mycobacterial agents
[作者:Ponaire, S; Zingle, C; Tritsch, D; Grosdemange-Billiard, C; Rohmer, M,期刊:European Journal of Medicinal Chemistry, 页码:277-285 , 文章类型: Article,,卷期:2012年51-1]
- Since Mycobacterium tuberculosis sets up several multiple anti-tuberculosis drug resistance mechanisms, development of new drugs with innovative target is urgent. The methylerythritol phosphate pathway (MEP) involved in ...
- Design and synthesis of novel 5-phenyl-N-piperidine ethanone containing 4,5-dihydropyrazole derivatives as potential antitumor agents
[作者:Liu, XH; Li, J; Shi, JB; Song, BA; Qi, XB,期刊:European Journal of Medicinal Chemistry, 页码:294-299 , 文章类型: Article,,卷期:2012年51-1]
- A series of novel 5-phenyl-N-piperidine ethanone-4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassays demonstrated that compounds 4d, 4f, 7a and 7h occupied high antiprolifer...
- Activity of novel quinoxaline-derived chalcones on in vitro glioma cell proliferation (vol 48, pg 255, 2012)
[作者:Mielcke, TR; Mascarello, A; Filippi-Chiela, E; Zanin, RF; Lenz, G; Leal, PC; Chiaradia, LD; Yunes, RA; Nunes, RJ; Battastini, AMO; Morrone, FB; Camposa, MM,期刊:European Journal of Medicinal Chemistry, 页码:300-300 , 文章类型: Correction,,卷期:2012年51-1]
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- Tuberculosis: The drug development pipeline at a glance
[作者:Villemagne, B; Crauste, C; Flipo, M; Baulard, AR; Deprez, B; Willand, N,期刊:European Journal of Medicinal Chemistry, 页码:1-16 , 文章类型: Review,,卷期:2012年51-1]
- Tuberculosis is a major disease causing every year 1.8 million deaths worldwide and represents the leading cause of mortality resulting from a bacterial infection. Introduction in the 60's of first-line drug regimen resu...
- Design and synthesis of novel magnolol derivatives as potential antimicrobial and antiproliferative compounds
[作者:Jada, S; Doma, MR; Singh, PP; Kumar, S; Malik, F; Sharma, A; Khan, IA; Qazi, GN; Kumar, HMS,期刊:European Journal of Medicinal Chemistry, 页码:35-41 , 文章类型: Article,,卷期:2012年51-1]
- A series of novel magnolol derivatives were synthesised and evaluated for in vitro antimicrobial and antiproliferative activities. We found that most of the compounds were effective inhibitors of Staphylococcus aureus, M...
- Enaminones 12. An explanation of anticonvulsant activity and toxicity per Linus Pauling's clathrate hypothesis
[作者:Jackson, PL; Hanson, CD; Farrell, AK; Butcher, RJ; Stables, JP; Eddington, ND; Scott, KR,期刊:European Journal of Medicinal Chemistry, 页码:42-51 , 文章类型: Article,,卷期:2012年51-1]
- The x-ray crystal structure of 3-((5-methylisoxazol-3-yl)amino)-5-methylcyclohex-2-enone (12b) and 3((5-methylisoxazolyl-3-yl)amino)-5,5-dimethylcyclohex-2-enone (12c) were determined and correlated to their anticonvulsa...
- Synthesis and in vitro antiplasmodial activities of fluoroquinolone analogs
[作者:Dixit, SK; Mishra, N; Sharma, M; Singh, S; Agarwal, A; Awasthi, SK; Bhasin, VK,期刊:European Journal of Medicinal Chemistry, 页码:52-59 , 文章类型: Article,,卷期:2012年51-1]
- Fluoroquinolone analogs were synthesized by simple alkylation followed by click chemistry and evaluated for their antimalarial in vitro against chloroquine sensitive strain of Plasmodium falciparum while ciprofloxacin wa...
- Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors
[作者:Chen, XW; Zhan, P; Pannecouque, C; Balzarini, J; De Clercq, E; Liu, XY,期刊:European Journal of Medicinal Chemistry, 页码:60-66 , 文章类型: Article,,卷期:2012年51-1]
- A novel series of piperidine-substituted triazine derivatives have been synthesized and evaluated for anti-HIV activities in MT-4 cells. Most compounds displayed extremely promising activity against wildtype HIV-1 with E...
- Synthesis and biological activity of 23-ethylidene-26-hydroxy-22-oxocholestane derivatives from spirostanic sapogenins
[作者:Perez-Diaz, JOH; Rarova, L; Ocampo, JPM; Magana-Vergara, NE; Farfan, N; Strnad, M; Santillan, R,期刊:European Journal of Medicinal Chemistry, 页码:67-78 , 文章类型: Article,,卷期:2012年51-1]
- The synthesis and biological evaluation of three new cholestane frameworks of the type: (25R)-3 beta,16 beta-Diacetoxy-23-ethylidene-26-hydroxy-22-oxocholestane, starting from spirostanic sapogenins of the 25R series, is...
- Synthesis of novel spirooxindole derivatives by one pot multicomponent reaction and their antimicrobial activity
[作者:Bhaskar, G; Arun, Y; Balachandran, C; Saikumar, C; Perumal, PT,期刊:European Journal of Medicinal Chemistry, 页码:79-91 , 文章类型: Article,,卷期:2012年51-1]
- A series of novel spirooxindoles have been synthesized through 1,3-dipolar cycloaddition of an azomethine ylide generated from isatin and sarcosine or L-proline with the dipolarophile 1,4-naphthoquinone followed by spont...
- Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist
[作者:Nakamura, T; Asano, M; Sekiguchi, Y; Mizuno, Y; Tamaki, K; Nara, F; Kawase, Y; Yabe, Y; Nakai, D; Kamiyama, E; Urasaki-Kaneno, Y; Shimozato, T; Doi-Komuro, H; Kagari, T; Tomisato, W; Inoue, R; Nagasaki, M; Yuita, H; Oguchi-Oshima, K; Kaneko, R; Nishi, T,期刊:European Journal of Medicinal Chemistry, 页码:92-98 , 文章类型: Article,,卷期:2012年51-1]
- Modulators of sphingosine phosphate receptor-1 (S1P(1)) have recently been focused as a suppressant of autoimmunity. We have discovered a 4-ethylthiophene-based S1P(1) agonist 1-({4-Ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxa...
- A novel anti-tumor agent, Ln(III) 2-thioacetate benzothiazole induces anti-angiogenic effect and cell death in cancer cell lines
[作者:Hussein, BHM; Azab, HA; El-Azab, MF; El-Falouji, AI,期刊:European Journal of Medicinal Chemistry, 页码:99-109 , 文章类型: Article,,卷期:2012年51-1]
- New complexes with a potent DNA-binding anti-tumor agent, europium(III)- and terbium(III)-2-thioacetate benzothiazole were synthesized and characterized. These complexes showed strong binding affinity to calf thymus DNA ...
- Studies on gambogic acid (IV): Exploring structure-activity relationship with I kappa B kinase-beta (IKK beta)
[作者:Sun, HP; Chen, FH; Wang, XJ; Liu, ZL; Yang, Q; Zhang, XJ; Zhu, J; Qiang, L; Guo, QL; You, QD,期刊:European Journal of Medicinal Chemistry, 页码:110-123 , 文章类型: Article,,卷期:2012年51-1]
- Previously we have reported a series of gambogic acid's analogs and have identified a compound that possessed comparable in vitro growth inhibitory effect as gambogic acid. However, their target protein as well as the ke...
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