- Design of Novel Cyclic Altered Peptide Ligands of Myelin Basic Protein MBP83-99 That Modulate Immune Responses in SJL/J Mice.
[作者:Katsara, Maria;Deraos, George;Tselios, Theodore;Matsoukas, John;Apostolopoulos, Vasso;,期刊:Journal of Medicinal Chemistry, 页码:3971-3978 , 文章类型: 研究论文,,卷期:2008年51-13]
- The use of antagonist peptides derived from the myelin sheath constitutes a promising therapeutic approach for multiple sclerosis (MS). Cyclization of peptide analogs is of great interest, since the limited stability of...
- Design and in Vitro Characterization of Highly sst2-Selective Somatostatin Antagonists Suitable for Radiotargeting.
[作者:Cescato, Renzo;Erchegyi, Judith;Waser, Beatrice;Piccand, Veronique;Maecke, Helmut R.;Rivier, Jean E.;Reubi, Jean Claude;,期刊:Journal of Medicinal Chemistry, 页码:4030-4037 , 文章类型: 研究论文,,卷期:2008年51-13]
- Radiolabeled sst2 and sst3 antagonists are better candidates for tumor targeting than agonists with comparable binding characteristics. Because most of the neuroendocrine tumors express sst2, we used the known antagonist...
- Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2- yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458).
[作者:Liu, Longbin;Siegmund, Aaron;Xi, Ning;Kaplan-Lefko, Paula;Rex, Karen;Chen, April;Lin, Jasmine;Moriguchi, Jodi;Berry, Loren;Huang, Liyue;Teffera, Yohannes;Yang, Yajing;Zhang, Yihong;Bellon, Steven F.;Lee, Matthew;Shimanovich, Roman;Bak, Annette;Dominguez,,期刊:Journal of Medicinal Chemistry, 页码:3688-3691 , 文章类型: 研究论文,,卷期:2008年51-13]
- Deregulation of the receptor tyrosine kinase c-Met has been implicated in human cancers. Pyrazolones with N-1 bearing a pendent hydroxyalkyl side chain showed selective inhibition of c-Met over VEGFR2. However, studies...
- Ensemble-Based Virtual Screening Reveals Potential Novel Antiviral Compounds for Avian Influenza Neuraminidase.
[作者:Cheng, Lily S.;Amaro, Rommie E.;Xu, Dong;Li, Wilfred W.;Arzberger, Peter W.;McCammon, J. Andrew;,期刊:Journal of Medicinal Chemistry, 页码:3878-3894 , 文章类型: 研究论文,,卷期:2008年51-13]
- Avian influenza virus subtype H5N1 is a potential pandemic threat with human-adapted strains resistant to antiviral drugs. Although virtual screening (VS) against a crystal or relaxed receptor structure is an establishe...
- Trithiocarbonates as a Novel Class of HDAC Inhibitors: SAR Studies, Isoenzyme Selectivity, and Pharmacological Profiles.
[作者:Dehmel, Florian;Weinbrenner, Steffen;Julius, Heiko;Ciossek, Thomas;Maier, Thomas;Stengel, Thomas;Fettis, Kamal;Burkhardt, Carmen;Wieland, Heike;Beckers, Thomas;,期刊:Journal of Medicinal Chemistry, 页码:3985-4001 , 文章类型: 研究论文,,卷期:2008年51-13]
- Inhibitors of histone deacetylases (HDAC) are currently developed for the treatment of cancer. These include compds. with a sulfur contg. head group like depsipeptide, alkylthiols, thiocarboxylates, and trithiocarbonate...
- Discovery of Novel, Potent Benzamide Inhibitors of 11b-Hydroxysteroid Dehydrogenase Type 1 (11b-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model.
[作者:Julian, Lisa D.;Wang, Zhulun;Bostick, Tracy;Caille, Seb;Choi, Rebekah;DeGraffenreid, Michael;Di, Yongmei;He, Xiao;Hungate, Randall W.;Jaen, Juan C.;Liu, Jinsong;Monshouwer, Mario;McMinn, Dustin;Rew, Yosup;Sudom, Athena;Sun, Daqing;Tu, Hua;Ursu, Stefania;W,期刊:Journal of Medicinal Chemistry, 页码:3953-3960 , 文章类型: 研究论文,,卷期:2008年51-13]
- The authors report the discovery of potent benzamide inhibitors of 11b-hydroxysteroid dehydrogenase (11b-HSD1). The optimization and correlation of in vitro and in vivo metabolic stability will be described. Through mo...
- Structure-Activity Relationships of 7-Deaza-6-benzylthioinosine Analogues as Ligands of Toxoplasma gondii Adenosine Kinase.
[作者:Kim, Young Ah;Sharon, Ashoke;Chu, Chung K.;Rais, Reem H.;Al Safarjalani, Omar N.;Naguib, Fardos N. M.;El Kouni, Mahmoud H.;,期刊:Journal of Medicinal Chemistry, 页码:3934-3945 , 文章类型: 研究论文,,卷期:2008年51-13]
- Several 7-deaza-6-benzylthioinosine analogs with varied substituents on arom. ring were synthesized and evaluated against Toxoplasma gondii adenosine kinase (EC.2.7.1.20). Structure-activity relationships indicated that...
- Brassinosteroids: Synthesis and Activity of Some Fluoro Analogues.
[作者:Slavikova, Barbora;Kohout, Ladislav;Budesinsky, Milos;Swaczynova, Jana;Kasal, Alexander;,期刊:Journal of Medicinal Chemistry, 页码:3979-3984 , 文章类型: 研究论文,,卷期:2008年51-13]
- contg. a fluorine atom in either the 3a or the 5a positions or in 3a and 5a positions, were prepd. using std. operations (reaction of 3b-alcs. with (diethylamino)sulfur trifluoride, cleavage of epoxide with HF in py or B...
- Sodium Late Current Blockers in Ischemia Reperfusion: Is the Bullet Magic?.
[作者:Le Grand, Bruno;Pignier, Christophe;Letienne, Robert;Cuisiat, Florence;Rolland, Francoise;Mas, Agnes;Vacher, Bernard;,期刊:Journal of Medicinal Chemistry, 页码:3856-3866 , 文章类型: 研究论文,,卷期:2008年51-13]
- We describe the discovery of the first selective, potent, and voltage-dependent inhibitor of the late current mediated by the cardiac sodium channel NaV1.5. The compd. 3,4-dihydro-N-[(2S)-3-[(2-methoxyphenyl)thio]-2-met...
- Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
[作者:Fookes, Christopher J. R.;Pham, Tien Q.;Mattner, Filomena;Greguric, Ivan;Loc'h, Christian;Liu, Xiang;Berghofer, Paula;Shepherd, Rachael;Gregoire, Marie-Claude;Katsifis, Andrew;,期刊:Journal of Medicinal Chemistry, 页码:3700-3712 , 文章类型: 研究论文,,卷期:2008年51-13]
- The fluoroethoxy and fluoropropoxy substituted (2-(6-chloro-2-phenyl)imidazo[1,2-a]pyridin-3-yl)-N,N-diethylacetamides I (n = 1) (PBR102) and I (n = 2) (PBR111) and (2-phenyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)-N,...
- A Novel Class of Cycloalkano[b]pyridines as Potent and Orally Active Opioid Receptor-like 1 Antagonists with Minimal Binding Affinity to the hERG K+ Channel.
[作者:Yoshizumi, Takashi;Takahashi, Hirobumi;Miyazoe, Hiroshi;Sugimoto, Yuichi;Tsujita, Tomohiro;Kato, Tetsuya;Ito, Hirokatsu;Kawamoto, Hiroshi;Hirayama, Mioko;Ichikawa, Daisuke;Azuma-Kanoh, Tomoko;Ozaki, Satoshi;Shibata, Yoshihiro;Tani, Takeshi;Chiba, Masato;I,期刊:Journal of Medicinal Chemistry, 页码:4021-4029 , 文章类型: 研究论文,,卷期:2008年51-13]
- A series of compds. based on 7-{[4-(2-methylphenyl)piperidin-1-yl]methyl}-6,7,8,9-tetrahydro-5H-cyclo hepta[b]pyridine-9-ol ((-)-I), a potent and selective opioid receptor-like 1 (ORL1) antagonist, was prepd. and evaluat...
- Design, Synthesis, and Evaluation of a Novel 4-Aminomethyl-4-fluoropiperidine as a T-Type Ca2+ Channel Antagonist.
[作者:Shipe, William D.;Barrow, James C.;Yang, Zhi-Qiang;Lindsley, Craig W.;Yang, F. Vivien;Schlegel, Kelly-Ann S.;Shu, Youheng;Rittle, Kenneth E.;Bock, Mark G.;Hartman, George D.;Tang, Cuyue;Ballard, Jeanine E.;Kuo, Yuhsin;Adarayan, Emily D.;Prueksaritanont, T,期刊:Journal of Medicinal Chemistry, 页码:3692-3695 , 文章类型: 研究论文,,卷期:2008年51-13]
- The novel T-type antagonist (S)-I has been prepd. and evaluated in in vitro and in vivo assays for T-type calcium ion channel activity. Structural modification of the piperidine leads afforded the fluorinated piperidine ...
- Synthesis and Pharmacological Characterization of Chiral Pyrrolidinylfuran Derivatives: The Discovery of New Functionally Selective Muscarinic Agonists.
[作者:Scapecchi, Serena;Nesi, Marta;Matucci, Rosanna;Bellucci, Cristina;Buccioni, Michela;Dei, Silvia;Guandalini, Luca;Manetti, Dina;Martini, Elisabetta;Marucci, Gabriella;Romanelli, Maria Novella;Teodori, Elisabetta;Cirilli, Roberto;,期刊:Journal of Medicinal Chemistry, 页码:3905-3912 , 文章类型: 研究论文,,卷期:2008年51-13]
- Building on the previously and successfully applied hypothesis that stereochem. complication in the proximity of the crit. cationic head of a cholinergic agonist would result in subtype selective compds., we synthesized ...
- Improvement of meta-tetra(Hydroxyphenyl)chlorin-Like Photosensitizer Selectivity with Folate-Based Targeted Delivery. Synthesis and in Vivo Delivery Studies.
[作者:Gravier, Julien;Schneider, Raphael;Frochot, Celine;Bastogne, Thierry;Schmitt, Frederic;Didelon, Jacques;Guillemin, Francois;Barberi-Heyob, Muriel;,期刊:Journal of Medicinal Chemistry, 页码:3867-3877 , 文章类型: 研究论文,,卷期:2008年51-13]
- (Biomolecules and Their Synthetic Analogs) Section The cell membrane folate receptor (FR) is a mol. target for tumor-selective drug delivery, including delivery of photosensitizers for anticancer photodynamic therapy (PD...
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