- Morpholino, Piperidino, and Pyrrolidino Derivatives of Pyrimidine Nucleosides as Inhibitors of Ribonuclease A: Synthesis, Biochemical, and Crystallographic Evaluation,.
[作者:Samanta, Anirban;Leonidas, Demetres D.;Dasgupta, Swagata;Pathak, Tanmaya;Zographos, Spyros E.;Oikonomakos, Nikos G.;,期刊:Journal of Medicinal Chemistry, 页码:932-942 , 文章类型: 研究论文,,卷期:2009年52-4]
- Six 5'-deoxy-5'-morpholine, piperidine, and pyrrolidine of pyrimidine nucleosides, e.g. I, have been synthesized and characterized. Their inhibitory action to RNase A has been studied by biochem. anal. and X-ray crystal...
- Directed Discovery of Agents Targeting the Met Tyrosine Kinase Domain by Virtual Screening.
[作者:Peach, Megan L.;Tan, Nelly;Choyke, Sarah J.;Giubellino, Alessio;Athauda, Gagani;Burke, Terrence R., Jr.;Nicklaus, Marc C.;Bottaro, Donald P.;,期刊:Journal of Medicinal Chemistry, 页码:943-951 , 文章类型: 研究论文,,卷期:2009年52-4]
- Hepatocyte growth factor (HGF) is an important regulator of normal development and homeostasis, and dysregulated signaling through the HGF receptor, Met, contributes to tumorigenesis, tumor progression, and metastasis in...
- Transferring the Concept of Multinuclearity to Ruthenium Complexes for Improvement of Anticancer Activity.
[作者:Mendoza-Ferri, Maria G.;Hartinger, Christian G.;Mendoza, Marco A.;Groessl, Michael;Egger, Alexander E.;Eichinger, Rene E.;Mangrum, John B.;Farrell, Nicholas P.;Maruszak, Magdalena;Bednarski, Patrick J.;Klein, Franz;Jakupec, Michael A.;Nazarov, Alexey A.;S,期刊:Journal of Medicinal Chemistry, 页码:916-925 , 文章类型: 研究论文,,卷期:2009年52-4]
- Multinuclear platinum anticancer complexes are a proven option to overcome resistance of established anticancer compds. Transferring this concept to ruthenium complexes led to the synthesis of dinuclear Ru(II)-arene com...
- Glycolipids and Benzylammonium Lipids as Novel Antisepsis Agents: Synthesis and Biological Characterization.
[作者:Piazza, Matteo;Rossini, Clara;Della Fiorentina, Silvia;Pozzi, Chiara;Comelli, Francesca;Bettoni, Isabella;Fusi, Paola;Costa, Barbara;Peri, Francesco;,期刊:Journal of Medicinal Chemistry, 页码:1209-1213 , 文章类型: 研究论文,,卷期:2009年52-4]
- New glycolipids and a benzylammonium lipid were rationally designed by varying the chem. structure of a D-glucose-derived hit compd. active as lipid A antagonist. The synthesis of these compds. is reported, and their in...
- First Cdc7 kinase inhibitors: Pyrrolopyridinones as potent and orally active antitumor agents. 2. lead discovery.
[作者:Menichincheri, Maria;Bargiotti, Alberto;Berthelsen, Jens;Bertrand, Jay A.;Bossi, Roberto;Ciavolella, Antonella;Cirla, Alessandra;Cristiani, Cinzia;Croci, Valter;D'Alessio, Roberto;Fasolini, Marina;Fiorentini, Francesco;Forte, Barbara;Isacchi, Antonella;Ma,期刊:Journal of Medicinal Chemistry, 页码:1230-1230 , 文章类型: 研究论文,,卷期:2009年52-4]
- On page 293, the Author line is incorrect due to incorrect affiliation superscript symbols; the correct symbols and versions of the Author and Affiliation lines are given.
- A Series of 2,4-Disubstituted Quinolines as a New Class of Allosteric Enhancers of the Adenosine A3 Receptor.
[作者:Heitman, Laura H.;Goeblyos, Aniko;Zweemer, Annelien M.;Bakker, Renee;Mulder-Krieger, Thea;van Veldhoven, Jacobus P. D.;de Vries, Henk;Brussee, Johannes;IJzerman, Adriaan P.;,期刊:Journal of Medicinal Chemistry, 页码:926-931 , 文章类型: 研究论文,,卷期:2009年52-4]
- The adenosine receptor subfamily consists of the adenosine A1, A2A, A2B, and A3 receptors, which are localized in a variety of tissues throughout the human body. It is, therefore, a challenge to develop receptor specifi...
- Total Synthesis of Photoactivatable or Fluorescent Anandamide Probes: Novel Bioactive Compounds with Angiogenic Activity.
[作者:Balas, Laurence;Durand, Thierry;Saha, Sattyabrata;Johnson, Inneke;Mukhopadhyay, Somnath;,期刊:Journal of Medicinal Chemistry, 页码:1005-1017 , 文章类型: 研究论文,,卷期:2009年52-4]
- Endocannabinoids are endogenous polyunsatd. fatty acids involved in a multitude of health and disease processes. Recently, several lines of evidence suggest the presence of a novel non-CB1/CB2 anandamide receptor in end...
- Structure-Activity Relationship Analysis of Novel Derivatives of Narciclasine (an Amaryllidaceae Isocarbostyril Derivative) as Potential Anticancer Agents.
[作者:Ingrassia, Laurent;Lefranc, Florence;Dewelle, Janique;Pottier, Laurent;Mathieu, Veronique;Spiegl-Kreinecker, Sabine;Sauvage, Sebastien;El Yazidi, Mohamed;Dehoux, Mischael;Berger, Walter;Van Quaquebeke, Eric;Kiss, Robert;,期刊:Journal of Medicinal Chemistry, 页码:1100-1114 , 文章类型: 研究论文,,卷期:2009年52-4]
- Narciclasine (1)(I) is a plant growth regulator that has been previously demonstrated to be proapoptotic to cancer cells at high concns. (? mM). Data generated in the present study show that narciclasine displays potent...
- Discovery of XL335 (WAY-362450), a Highly Potent, Selective, and Orally Active Agonist of the Farnesoid X Receptor (FXR).
[作者:Flatt, Brenton;Martin, Richard;Wang, Tie-Lin;Mahaney, Paige;Murphy, Brett;Gu, Xiao-Hui;Foster, Paul;Li, Jiali;Pircher, Parinaz;Petrowski, Mary;Schulman, Ira;Westin, Stefan;Wrobel, Jay;Yan, Grace;Bischoff, Eric;Daige, Chris;Mohan, Raju;,期刊:Journal of Medicinal Chemistry, 页码:904-907 , 文章类型: 研究论文,,卷期:2009年52-4]
- Azepino[4,5-b]indoles have been identified as potent agonists of the farnesoid X receptor (FXR). In vitro and in vivo optimization has led to the discovery of 6m (XL335, WAY-362450) as a potent, selective, and orally bi...
- Discovery of the First Selective Inhibitor of Excitatory Amino Acid Transporter Subtype 1.
[作者:Jensen, Anders A.;Erichsen, Mette N.;Nielsen, Christina W.;Stensboel, Tine B.;Kehler, Jan;Bunch, Lennart;,期刊:Journal of Medicinal Chemistry, 页码:912-915 , 文章类型: 研究论文,,卷期:2009年52-4]
- The discovery of the first class of subtype-selective inhibitors of the human excitatory amino acid transporter subtype 1 (EAAT1) and its rat orthologue GLAST is reported. An opening structure-activity relationship of 2...
- Structure-Based Drug Design of Novel Aurora Kinase A Inhibitors: Structural Basis for Potency and Specificity.
[作者:Coumar, Mohane Selvaraj;Leou, Jiun-Shyang;Shukla, Paritosh;Wu, Jian-Sung;Dixit, Ajay Kumar;Lin, Wen-Hsing;Chang, Chun-Yu;Lien, Tzu-Wen;Tan, Uan-Kang;Chen, Chun-Hwa;Hsu, John T.-A.;Chao, Yu-Sheng;Wu, Su-Ying;Hsieh, Hsing-Pang;,期刊:Journal of Medicinal Chemistry, 页码:1050-1062 , 文章类型: 研究论文,,卷期:2009年52-4]
- Aurora kinases have emerged as attractive targets for the design of anticancer drugs. Through structure-based virtual screening, novel pyrazole hit 8a was identified as Aurora kinase A inhibitor (IC50 = 15.1 mM). X-ray...
- Discovery and Structure-Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists.
[作者:Yang, Wu;Ruan, Zheming;Wang, Yufeng;Van Kirk, Katy;Ma, Zhengping;Arey, Brian J.;Cooper, Christopher B.;Seethala, Ramakrishna;Feyen, Jean H. M.;Dickson, John K.;,期刊:Journal of Medicinal Chemistry, 页码:1204-1208 , 文章类型: 研究论文,,卷期:2009年52-4]
- The trisubstituted pyrimidine I was identified through high-throughput screening as a novel calcium-sensing receptor (CaSR) antagonist. Small mol. CaSR antagonists and/or neg. allosteric modulators have the potential to ...
- Probes for Narcotic Receptor Mediated Phenomena. 37. Synthesis and Opioid Binding Affinity of the Final Pair of Oxide-Bridged Phenylmorphans, the Ortho- and Para-b-Isomers and Their N-Phenethyl Analogues, and the Synthesis of the N-Phenethyl Analogues of
[作者:Kurimura, Muneaki;Liu, Hehua;Sulima, Agnieszka;Hashimoto, Akihiro;Przybyl, Anna K.;Ohshima, Etsuo;Kodato, Shinichi;Deschamps, Jeffrey R.;Dersch, Christina M.;Rothman, Richard B.;Lee, Yong Sok;Jacobson, Arthur E.;Rice, Kenner C.;,期刊:Journal of Medicinal Chemistry, 页码:1229-1229 , 文章类型: 研究论文,,卷期:2009年52-4]
- On page 7868, in column 1, the sentence just before the first full paragraph should read: "The structure of 20 was established by single crystal X-ry crystallog. (Figure 3).". On page 7868, the sentence preceding th "Re...
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