- New Selective Inhibitors of Steroid 11b-Hydroxylation in the Adrenal Cortex. Synthesis and Structure-Activity Relationship of Potent Etomidate Analogues.
[作者：Zolle, Ilse M.;Berger, Michael L.;Hammerschmidt, Friedrich;Hahner, Stefanie;Schirbel, Andreas;Peric-Simov, Biljana;,期刊：Journal of Medicinal Chemistry, 页码：7652-7652 , 文章类型： 研究论文，,卷期：2008年51-23]
- The authors dicuss how research by Hanher et al., (2008) afects their research involving 123I-iodometomidate as a mol. imager.
- Design, Synthesis, and Evaluation of Tricyclic, Conformationally Constrained Small-Molecule Mimetics of Second Mitochondria-Derived Activator of Caspases.
[作者：Zhang, Bin;Nikolovska-Coleska, Zaneta;Zhang, Yan;Bai, Longchuan;Qiu, Su;Yang, Chao-Yie;Sun, Haiying;Wang, Shaomeng;Wu, Yikang;,期刊：Journal of Medicinal Chemistry, 页码：7352-7355 , 文章类型： 研究论文，,卷期：2008年51-23]
- A series of tricyclic, conformationally constrained Smac mimetics have been designed, synthesized, and evaluated. The most potent compd. 6 (WS-5) binds to XIAP, cIAP-1, and cIAP-2 with Ki of 18, 1.1, and 4.2 nM, resp. ...
- Synthesis and Pharmacological Characterization of Novel Druglike Corticotropin-Releasing Factor 1 Antagonists.
[作者：Di Fabio, Romano;St-Denis, Yves;Sabbatini, Fabio M.;Andreotti, Daniele;Arban, Roberto;Bernasconi, Giovanni;Braggio, Simone;Blaney, Frank E.;Capelli, Anna M.;Castiglioni, Emiliano;Di Modugno, Enza;Donati, Daniele;Fazzolari, Elettra;Ratti, Emiliangelo;Feria,期刊：Journal of Medicinal Chemistry, 页码：7370-7379 , 文章类型： 研究论文，,卷期：2008年51-23]
- To identify new CRF1 receptor antagonists, an attempt to modify the bis-heterocycle moiety present in the top region of the dihydropyrrole[2,3]pyridine template was made following new pharmacophoric hypothesis on the CRF...
- Targeting the Delivery of Glycan-Based Paclitaxel Prodrugs to Cancer Cells via Glucose Transporters.
[作者：Lin, Yih-Shyan;Tungpradit, Rudeewan;Sinchaikul, Supachok;An, Feng-Ming;Liu, Der-Zen;Phutrakul, Suree;Chen, Shui-Tein;,期刊：Journal of Medicinal Chemistry, 页码：7428-7441 , 文章类型： 研究论文，,卷期：2008年51-23]
- This report describes the synthesis of four novel paclitaxel based prodrugs with glycan conjugation. Glycans were conjugated using an ester or ether bond as the linker between 2'-paclitaxel and the 2'-glucose or glucuro...
- Novel Bis- and Tris-1,2,4-trioxanes: Synthesis and Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii in Swiss Mice.
[作者：Singh, Chandan;Verma, Ved Prakash;Naikade, Niraj Krishna;Singh, Ajit Shankar;Hassam, Mohammad;Puri, Sunil K.;,期刊：Journal of Medicinal Chemistry, 页码：7581-7592 , 文章类型： 研究论文，,卷期：2008年51-23]
- A new series of bis-1,2,4-trioxanes and tris-1,2,4-trioxanes were prepd. and evaluated against multidrug-resistant Plasmodium yoelii in Swiss mice by oral route. Five cyclopentane-based bis-trioxanes and three cyclohexa...
- Triazine Compounds as Antagonists at Bv8-Prokineticin Receptors.
[作者：Balboni, Gianfranco;Lazzari, Ilaria;Trapella, Claudio;Negri, Lucia;Lattanzi, Roberta;Giannini, Elisa;Nicotra, Annalisa;Melchiorri, Pietro;Visentin, Sergio;De Nuccio, Chiara;Salvadori, Severo;,期刊：Journal of Medicinal Chemistry, 页码：7635-7639 , 文章类型： 研究论文，,卷期：2008年51-23]
- We approached a new synthesis of some 1,3,5-triazine-4,6-diones as potential non peptidic prokineticin receptor antagonists, contg. the following substitutions: N1 and N5 are linked to 4-methoxybenzyl and 4-ethylbenzyl g...
- 2-[(3-Methoxyphenylethyl)phenoxy]-Based ABCB1 Inhibitors: Effect of Different Basic Side-Chains on Their Biological Properties.
[作者：Colabufo, Nicola Antonio;Berardi, Francesco;Perrone, Roberto;Rapposelli, Simona;Digiacomo, Maria;Vanni, Michael;Balsamo, Aldo;,期刊：Journal of Medicinal Chemistry, 页码：7602-7613 , 文章类型： 研究论文，,卷期：2008年51-23]
- Recently, the 2-[(3-methoxyphenylethyl)phenoxy] moiety has been selected for the design and synthesis of new small ABCB1 inhibitors. In the present paper, this moiety has been linked through a spacer of 2-5 carbon atoms ...
- Surprising Alteration of Antibacterial Activity of 5''-Modified Neomycin against Resistant Bacteria.
[作者：Zhang, Jianjun;Chiang, Fang-I.;Wu, Long;Czyryca, Przemyslaw Greg;Li, Ding;Chang, Cheng-Wei Tom;,期刊：Journal of Medicinal Chemistry, 页码：7563-7573 , 文章类型： 研究论文，,卷期：2008年51-23]
- A facile synthetic protocol for the prodn. of neomycin B derivs. with various modifications at the 5'' position has been developed. The structural activity relation (SAR) against aminoglycoside resistant bacteria equipp...
- Inhibition of Siderophore Biosynthesis by 2-Triazole Substituted Analogues of 5'-O-[N-(Salicyl)sulfamoyl]adenosine: Antibacterial Nucleosides Effective against Mycobacterium tuberculosis.
[作者：Gupte, Amol;Boshoff, Helena I.;Wilson, Daniel J.;Neres, Joao;Labello, Nicholas P.;Somu, Ravindranadh V.;Xing, Chengguo;Barry, Clifton E.;Aldrich, Courtney C.;,期刊：Journal of Medicinal Chemistry, 页码：7495-7507 , 文章类型： 研究论文，,卷期：2008年51-23]
- The synthesis, biochem., and biol. evaluation of a systematic series of 2-triazole derivs. of 5'-O-[N-(salicyl)sulfamoyl]adenosine (Sal-AMS) are described as inhibitors of aryl acid adenylating enzymes (AAAE) involved in...
- Synthetic and Crystallographic Studies of a New Inhibitor Series Targeting Bacillus anthracis Dihydrofolate Reductase.
[作者：Beierlein, Jennifer M.;Frey, Kathleen M.;Bolstad, David B.;Pelphrey, Phillip M.;Joska, Tammy M.;Smith, Adrienne E.;Priestley, Nigel D.;Wright, Dennis L.;Anderson, Amy C.;,期刊：Journal of Medicinal Chemistry, 页码：7532-7540 , 文章类型： 研究论文，,卷期：2008年51-23]
- Bacillus anthracis, the causative agent of anthrax, poses a significant biodefense danger. Serious limitations in approved therapeutics and the generation of resistance have produced a compelling need for new therapeuti...
- Identification of G protein-coupled receptor 120-selective agonists derived from PPARg agonists.
[作者：Suzuki, Takayoshi;Igari, Sou-ichi;Hirasawa, Akira;Hata, Mie;Ishiguro, Masaji;Fujieda, Hiroki;Itoh, Yukihiro;Hirano, Tatsuya;Nakagawa, Hidehiko;Ogura, Michitaka;Makishima, Makoto;Tsujimoto, Gozoh;Miyata, Naoki;,期刊：Journal of Medicinal Chemistry, 页码：7640-7644 , 文章类型： 研究论文，,卷期：2008年51-23]
- A weak, nonselective G protein-coupled receptor 120 (GPR120) agonist 10 was found by screening a series of carboxylic acids derived from the peroxisome proliferator-activated receptor g (PPARg) agonist 3. Modification b...
- Design of Annulated Pyrazoles as Inhibitors of HIV-1 Reverse Transcriptase.
[作者：Sweeney, Zachary K.;Harris, Seth F.;Arora, Nidhi;Javanbakht, Hassan;Li, Yu;Fretland, Jennifer;Davidson, James P.;Billedeau, J. Roland;Gleason, Shelley K.;Hirschfeld, Donald;Kennedy-Smith, Joshua J.;Mirzadegan, Taraneh;Roetz, Ralf;Smith, Mark;Sperry, Sarah,期刊：Journal of Medicinal Chemistry, 页码：7449-7458 , 文章类型： 研究论文，,卷期：2008年51-23]
- Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are recommended components of preferred combination antiretroviral therapies used for the treatment of HIV. These regimens are extremely effective in suppressing ...
- Antitumor activity of new substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and 3-(5-imidazo[2,1-b]thiadiazolylmethylene)-2-indolinones: selectivity against colon tumor cells and effect on cell cycle-related events.
[作者：Andreani, Aldo;Burnelli, Silvia;Granaiola, Massimiliano;Leoni, Alberto;Locatelli, Alessandra;Morigi, Rita;Rambaldi, Mirella;Varoli, Lucilla;Calonghi, Natalia;Cappadone, Concettina;Voltattorni, Manuela;Zini, Maddalena;Stefanelli, Claudio;Masotti, Lanfranco,期刊：Journal of Medicinal Chemistry, 页码：7508-7513 , 文章类型： 研究论文，,卷期：2008年51-23]
- The synthesis of new 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones and 3-(5-imidazo[2,1-b]thiadiazolylmethylene)-2-indolinones is reported. The antitumor activity was evaluated according to the protocols available...
- In Pursuit of Natural Product Leads: Synthesis and Biological Evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazol e-4-carboxylic acid (A-33853) and Its Analogues: Discovery of N-(2-Benzoxazol-2-ylphenyl)benzamides as Novel
[作者：Tipparaju, Suresh K.;Joyasawal, Sipak;Pieroni, Marco;Kaiser, Marcel;Brun, Reto;Kozikowski, Alan P.;,期刊：Journal of Medicinal Chemistry, 页码：7344-7347 , 文章类型： 研究论文，,卷期：2008年51-23]
- The antibiotic A 33853 I (R = 3-hydroxy-2-pyridinyl; R1 = HO), an acylaminophenylbenzooxazolecarboxylic acid, a potential antileishmanial agent, is prepd. for the first time; analogous acylaminophenylbenzooxazolecarboxyl...
- Development of Novel G-Protein-Coupled Receptor 54 Agonists with Resistance to Degradation by Matrix Metalloproteinase.
[作者：Tomita, Kenji;Oishi, Shinya;Ohno, Hiroaki;Peiper, Stephen C.;Fujii, Nobutaka;,期刊：Journal of Medicinal Chemistry, 页码：7645-7649 , 文章类型： 研究论文，,卷期：2008年51-23]
- Kisspeptin-GPR54 signaling is involved in the suppression of cancer metastasis and regulation of hormonal secretion. Recently, matrix metalloproteinase mediated deactivation of kisspeptins through hydrolysis of the Gly-...
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