- Synthesis, human monoamine oxidase inhibitory activity and molecular docking studies of 3-heteroarylcoumarin derivatives
[作者:Delogu, G; Picciau, C; Ferino, G; Quezada, E; Podda, G; Uriarte, E; Vina, D,期刊:European Journal of Medicinal Chemistry, 页码:1147-1152 , 文章类型: Article,,卷期:2011年46-4]
- Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. Series of 3-indolyl and 3-thiophenylcoumarins were synthesized and evaluated as inhibitors of the two human MAO isoforms, h...
- Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents
[作者:You, H; Youn, HS; Im, I; Bae, MH; Lee, SK; Ko, H; Eom, SH; Kim, YC,期刊:European Journal of Medicinal Chemistry, 页码:1153-1164 , 文章类型: Article,,卷期:2011年46-4]
- NAmPRTase (PBEF/Visfatin) plays a pivotal role in the salvage pathway of NAD(+) biosynthesis. NAmPRTase has been an attractive target for anti-cancer agents that induce apoptosis of tumor cells via a declining plasma NAD...
- Structure-activity relationship of 2,4,5-trioxoimidazolidines as inhibitors of thymidine phosphorylase
[作者:Rajabi, M; Mansell, D; Freeman, S; Bryce, RA,期刊:European Journal of Medicinal Chemistry, 页码:1165-1171 , 文章类型: Article,,卷期:2011年46-4]
- Novel non-nucleobase-derived inhibitors of the angiogenic enzyme, thymidine phosphorylase, have been identified using molecular modelling, synthesis and biological evaluation. These inhibitors are 2,4,5-trioxoimidazolidi...
- Biological evaluation of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imine derivatives
[作者:Huang, C; Yan, SJ; Zeng, XH; Dai, XY; Zhang, Y; Qing, C; Lin, J,期刊:European Journal of Medicinal Chemistry, 页码:1172-1180 , 文章类型: Article,,卷期:2011年46-4]
- A series of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imines were evaluated in vitro against human tumour cell lines including A431, K562, HL60, HepG2 and Skov-3. As a result, some of the target compounds suc...
- 2-Substituted 5,6-dimethyl-3-phenylsulfonyl-pyrazolo[1,5-a]pyrimidines: New series of highly potent and specific serotonin 5-HT6 receptor antagonists
[作者:Ivachtchenko, AV; Golovina, ES; Kadieva, MG; Koryakova, AG; Mitkin, OD; Tkachenko, SE; Kysil, VM; Okun, I,期刊:European Journal of Medicinal Chemistry, 页码:1189-1197 , 文章类型: Article,,卷期:2011年46-4]
- Syntheses, biological evaluation, and structure activity relationships for a series of novel 2-substituted 3-benzenesulfonyl-5,6-dimethyl-pyrazolo[1,5-a]pyrimidines are disclosed. In spite of a wide, four orders of magni...
- Feruloylacetone as the model compound of half-curcumin: Synthesis and antioxidant properties
[作者:Feng, JY; Liu, ZQ,期刊:European Journal of Medicinal Chemistry, 页码:1198-1206 , 文章类型: Article,,卷期:2011年46-4]
- In order to clarify the contribution of phenolic and enolic hydroxyl group to the antioxidant capacity of feruloylacetone, a model compound of half-curcumin, 6-(p-hydroxy-m-methoxyphenyl)-5-hexene-2,4-dione (FT), 6-(p-be...
- Synthesis and pharmacological evaluation of bivalent antagonists of the nociceptin opioid receptor
[作者:Del Giudice, MR; Borioni, A; Bastanzio, G; Sbraccia, M; Mustazza, C; Sestili, I,期刊:European Journal of Medicinal Chemistry, 页码:1207-1221 , 文章类型: Article,,卷期:2011年46-4]
- Bivalent ligands constituted by two identical pharmacophores structurally related to the Nociceptin Opioid Receptor (NOPr) antagonist JTC-801 were synthesized and their binding affinities for NOPr were evaluated. The nov...
- Antioxidant xanthone derivatives induce cell cycle arrest and apoptosis and enhance cell death induced by cisplatin in NTUB1 cells associated with ROS
[作者:Cheng, JH; Huang, AM; Hour, TC; Yang, SC; Pu, YS; Lin, CN,期刊:European Journal of Medicinal Chemistry, 页码:1222-1231 , 文章类型: Article,,卷期:2011年46-4]
- In an effort to develop novel antioxidant as anticancer agents, a series of xanthones were prepared. In vitro screening, the synthetic xanthones revealed significant inhibitory effects on xanthine oxidase and ABTS radica...
- Synthesis and antibacterial evaluation of novel 8-fluoro Norfloxacin derivatives as potential probes for methicillin and vancomycin-resistant Staphylococcus aureus
[作者:Sunduru, N; Gupta, L; Chauhan, K; Mishra, NN; Shukla, PK; Chauhan, PMS,期刊:European Journal of Medicinal Chemistry, 页码:1232-1244 , 文章类型: Article,,卷期:2011年46-4]
- A series of novel 8-fluoro Norfloxacin derivatives and the hybrids of its piperazinyl derivatives incorporated with 1,3,5-triazine and pyrimidine were synthesized. All the above compounds were evaluated for their antibac...
- Structure-based design and biological profile of (E)-N-(4-Nitrobenzylidene)-2-naphthohydrazide, a novel small molecule inhibitor of I kappa B kinase-beta
[作者:Avila, CM; Lopes, AB; Goncalves, AS; da Silva, LL; Romeiro, NC; Miranda, ALP; Sant'Anna, CMR; Barreiro, EJ; Fraga, CAM,期刊:European Journal of Medicinal Chemistry, 页码:1245-1253 , 文章类型: Article,,卷期:2011年46-4]
- In this study, we describe the rational design, molecular modeling and pharmacological profile of a novel IKK-beta inhibitor (E)-N-(4-nitrobenzylidene)-2-naphthohydrazide (LASSBio-1524). The design based on the IKK-beta ...
- Synthesis and innate immunosuppressive effect of 1,2-cyclopentanediol derivatives
[作者:Kikuchi, H; Okazaki, K; Sekiya, M; Uryu, Y; Ueda, K; Katou, Y; Kurata, S; Oshima, Y,期刊:European Journal of Medicinal Chemistry, 页码:1263-1273 , 文章类型: Article,,卷期:2011年46-4]
- Innate immunity is the front line of self-defense against infectious microorganisms. In mammals, innate immunity interacts with adaptive immunity and plays a key role in regulating the immune response. Therefore, innate ...
- The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: Synthesis, cytotoxicity, DNA intercalation and photocleavage
[作者:Li, XL; Lin, YJ; Wang, QQ; Yuan, YK; Zhang, H; Qian, XH,期刊:European Journal of Medicinal Chemistry, 页码:1274-1279 , 文章类型: Article,,卷期:2011年46-4]
- A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing "click reaction". For anti-tumor activity in vitro, all the compounds were found to be more toxic...
- Studies on chemical modification and biology of a natural product, gambogic acid (III): Determination of the essential pharmacophore for biological activity
[作者:Wang, XJ; Lu, N; Yang, QA; Gong, DD; Lin, CJ; Zhang, SL; Xi, MY; Gao, YA; Wei, LB; Guo, QL; You, QD,期刊:European Journal of Medicinal Chemistry, 页码:1280-1290 , 文章类型: Article,,卷期:2011年46-4]
- Caged 4-oxa-tricyclo[4.3.1.0(3,7)]dec-2-one structural motifs are found in Garcinia natural products that demonstrate anti-tumor activity. Gambogic acid (GA, 1), the most abundant caged Garcinia xanthones, has been repor...
- Synthesis and anti-inflammatory activity of ent-kaurene derivatives
[作者:Hueso-Falcon, I; Cuadrado, I; Cidre, F; Amaro-Luis, JM; Ravelo, AG; Estevez-Braun, A; de las Heras, BD; Hortelano, S,期刊:European Journal of Medicinal Chemistry, 页码:1291-1305 , 文章类型: Article,,卷期:2011年46-4]
- A series of kaurene derivatives (1-63) were prepared and evaluated for anti-inflammatory activity. Thirteen of the tested compounds were able to inhibit NO production wits an IC50 between 2 and 10 mu M. Compounds 11, 12,...
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