- Synthesis and biological evaluation of cyclopentane-linked alkyl phosphocholines as potential anticancer agents that act by inhibiting Akt phosphorylation
[作者:Alam, MM; Joh, EH; Kim, Y; Oh, YI; Hong, J; Kim, B; Kim, DH; Lee, YS,期刊:European Journal of Medicinal Chemistry, 页码:485-492 , 文章类型: Article,,卷期:2012年47-1]
- Three new series of novel alkylphosphocholine (APC) derivatives containing a cyclopentane ring near the phosphocholine head group were synthesized. In the first set of analogues, the phosphocholine head group was attache...
- Fragment based lead discovery of small molecule inhibitors for the EPHA4 receptor tyrosine kinase
[作者:van Linden, OPJ; Farenc, C; Zoutman, WH; Hameetman, L; Wijtmans, M; Leurs, R; Tensen, CP; Siegal, G; de Esch, IJP,期刊:European Journal of Medicinal Chemistry, 页码:493-500 , 文章类型: Article,,卷期:2012年47-1]
- The in silica identification, optimization and crystallographic characterization of a 6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinolin-1-amine scaffold as an inhibitor for the EPHA4 receptor tyrosine kinase is described....
- Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker
[作者:Piotrowska, DG; Balzarini, J; Glowacka, IE,期刊:European Journal of Medicinal Chemistry, 页码:501-509 , 文章类型: Article,,卷期:2012年47-1]
- Azidation (TMSN(3), SnCl(4)) of a 9:1 mixture of trans- and cis-5-acetoxy-2-methylisoxazolidin-3-yl-3-phosphonates at the anomeric carbon atom led to the formation of the equimolar mixture of cis- and trans-5-azido-2-met...
- New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds
[作者:Faist, J; Seebacher, W; Saf, R; Brun, R; Kaiser, M; Weis, R,期刊:European Journal of Medicinal Chemistry, 页码:510-519 , 文章类型: Article,,卷期:2012年47-1]
- The 4-methylpiperazinyl group was inserted as substituent at the bridgehead of bicyclic compounds or as terminal group of their aminoacyl and aminoalkyl side chains. The new compounds were tested in vitro for their activ...
- New potent 5-HT(2A) receptor ligands containing an N '-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation
[作者:Fiorino, F; Severino, B; Magli, E; Perissutti, E; Frecentese, F; Esposito, A; Incisivo, GM; Ciano, A; Massarelli, P; Nencini, C; Santagada, V; Caliendo, G,期刊:European Journal of Medicinal Chemistry, 页码:520-529 , 文章类型: Article,,卷期:2012年47-1]
- N'-cyanopicolinamidine derivatives, linked to an arylpiperazine moiety, were prepared and their affinity to serotonin 5-HT(2A) and 5-HT(2c) receptors were evaluated. The combination of structural elements (heterocyclic n...
- Synthesis and anticancer activity of 4 beta-alkylamidochalcone and 4 beta-cinnamido linked podophyllotoxins as apoptotic inducing agents
[作者:Kamal, A; Mallareddy, A; Suresh, P; Nayak, VL; Shetti, RVCRNC; Rao, NS; Tamboli, JR; Shaik, TB; Vishnuvardhan, MVPS; Ramakrishna, S,期刊:European Journal of Medicinal Chemistry, 页码:530-545 , 文章类型: Article,,卷期:2012年47-1]
- A series of 4 beta-alkylamidochalcone and 4 beta-cinnamido linked podophyllotoxin congeners have been synthesized. All the twenty nine compounds were evaluated for anticancer activity against five human cancer cell lines...
- PEG-SO(3)H catalyzed synthesis and cytotoxicity of alpha-aminophosphonates
[作者:Reddy, CB; Kumar, KS; Kumar, MA; Reddy, MVN; Krishna, BS; Naveen, M; Arunasree, MK; Reddy, CS; Raju, CN; Reddy, CD,期刊:European Journal of Medicinal Chemistry, 页码:553-559 , 文章类型: Article,,卷期:2012年47-1]
- One pot three-component PEG-SO(3)H catalyzed reaction of 4-(Pyridin-4-yl)benzaldehyde and triethyl phosphite with various primary amines afforded alpha-aminophosphonates with high yields by the Kabachnik-Field's reaction...
- Dendrimer-based multivalent methotrexates as dual acting nanoconjugates for cancer cell targeting
[作者:Li, MH; Choi, SK; Thomas, TP; Desai, A; Lee, KH; Kotlyar, A; Holl, MMB; Baker, JR,期刊:European Journal of Medicinal Chemistry, 页码:560-572 , 文章类型: Article,,卷期:2012年47-1]
- Cancer-targeting drug delivery can be based on the rational design of a therapeutic platform. This approach is typically achieved by the functionalization of a nanoparticle with two distinct types of molecules, a targeti...
- N-Aryl-2-phenyl-2,3-dihydro-imidazo[1,2-b]pyrazole-1-carboxamides 7-substituted strongly inhibiting both fMLP-OMe- and IL-8-induced human neutrophil chemotaxis
[作者:Brullo, C; Spisani, S; Selvatici, R; Bruno, O,期刊:European Journal of Medicinal Chemistry, 页码:573-579 , 文章类型: Article,,卷期:2012年47-1]
- Anomalous activation of neutrophil recruitment is one of the causes of many inflammatory diseases. The chemoattractants N-formyl-methionyl-leucyl-phenylalanine (fMLP), and interleukine 8 (IL8) play a pivotal role in neut...
- Studies on the synthesis and antibacterial activity of 3,6-disubstituted 1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles
[作者:Plech, T; Wujec, M; Kosikowska, U; Malm, A; Kapron, B,期刊:European Journal of Medicinal Chemistry, 页码:580-584 , 文章类型: Article,,卷期:2012年47-1]
- Treating infections caused by drug-resistant bacterial strains constitutes one of the most essential challenges for medicine nowadays. A range of new derivatives of 1,2,4-triazolo[3,4-b]1,3,4-thiadiazole have been synthe...
- 1,2,3-Triazole tethered beta-lactam-Chalcone bifunctional hybrids: Synthesis and anticancer evaluation
[作者:Singh, P; Raj, R; Kumar, V; Mahajan, MP; Bedi, PMS; Kaur, T; Saxena, AK,期刊:European Journal of Medicinal Chemistry, 页码:594-600 , 文章类型: Article,,卷期:2012年47-1]
- The manuscript describes the synthesis of novel 1,2,3-triazole tethered beta-lactam-chalcone bifunctional hybrids via click chemistry approach utilizing azide-alkyne cycloaddition reactions and their evaluation as antica...
- A novel caryophyllene type sesquiterpene lactone from Asparagus falcatus (Linn.); Structure elucidation and anti-angiogenic activity on HUVECs
[作者:Ghalib, RM; Hashim, R; Sulaiman, O; Mehdi, SH; Valkonen, A; Rissanen, K; Trifunovic, SR; Ahamed, MBK; Majid, AMSA; Kawamura, F,期刊:European Journal of Medicinal Chemistry, 页码:601-607 , 文章类型: Article,,卷期:2012年47-1]
- In this study the novel caryophyllene type sesquiterpene lactone (aspfalcolide) has been isolated from the leaves of Asparagus falcatus (Linn.) and characterized by IR, 1D NMR, 2D NMR, El-MS, HR-ESI-MS and X-ray single c...
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