个性化文献订阅>文章检索

文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共34条记录   Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors. [作者：Kumar, Sanjeev;Malachowski, William P.;DuHadaway, James B.;LaLonde, Judith M.;Carroll, Patrick J.;Jaller, Daniel;Metz, Richard;Prendergast, George C.;Muller, Alexander J.;,期刊：Journal of Medicinal Chemistry, 页码：7325-7325 , 文章类型： 研究论文，,卷期：2008年51-22] On page 1712, in the left column, in paragraph 3, in line 9, "potent inhibitors (34, 39, and 50)", was incorrectly given, and should read: "potent inhibitors (36, 41, and 50)". Insights into Ligand-Elicited Activation of Human Constitutive Androstane Receptor Based on Novel Agonists and Three-Dimensional Quantitative Structure-Activity Relationship. [作者：Jyrkkaerinne, Johanna;Windshugel, Bjorn;Roenkkoe, Toni;Tervo, Anu J.;Kublbeck, Jenni;Lahtela-Kakkonen, Maija;Sippl, Wolfgang;Poso, Antti;Honkakoski, Paavo;,期刊：Journal of Medicinal Chemistry, 页码：7181-7192 , 文章类型： 研究论文，,卷期：2008年51-22] The human constitutive androstane receptor (CAR, NR1I3) is an important regulator of xenobiotic metab. and other physiol. processes. So far, only few CAR agonists are known and no explicit mechanism has been proposed for... From Ligand to Complexes. Part 2. Remarks on Human Immunodeficiency Virus type 1 Integrase Inhibition by b-Diketo Acid Metal Complexes. [作者：Bacchi, Alessia;Biemmi, Mariano;Carcelli, Mauro;Carta, Fabrizio;Compari, Carlotta;Fisicaro, Emilia;Rogolino, Dominga;Sechi, Mario;Sippel, Martin;Sotriffer, Christoph A.;Sanchez, Tino W.;Neamati, Nouri;,期刊：Journal of Medicinal Chemistry, 页码：7253-7264 , 文章类型： 研究论文，,卷期：2008年51-22] Previously, the authors synthesized a series of b-diketo acid metal complexes as novel HIV-1 integrase (IN) inhibitors (J. Med. Chem.2006, 46, 4248-4260). Herein, a further extension of this study is reported. First, d... Antithyroid Drug Carbimazole and Its Analogues: Synthesis and Inhibition of Peroxidase-Catalyzed Iodination of L-Tyrosine. [作者：Das, Debasis;Roy, Gouriprasanna;Mugesh, Govindasamy;,期刊：Journal of Medicinal Chemistry, 页码：7313-7317 , 文章类型： 研究论文，,卷期：2008年51-22] Synthesis and biol. activity of the antithyroid drug carbimazole (CBZ) and its analogs I (E = S, Se, R = Et, Me) are described. The introduction of an ethoxycarbonyl group in methimazole and its selenium analog not only... Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis. [作者：Wrobel, Jay;Steffan, Robert;Bowen, S. Marc;Magolda, Ronald;Matelan, Edward;Unwalla, Rayomand;Basso, Michael;Clerin, Valerie;Gardell, Stephen J.;Nambi, Ponnal;Quinet, Elaine;Reminick, Jason I.;Vlasuk, George P.;Wang, Shuguang;Feingold, Irene;Huselton, Chri,期刊：Journal of Medicinal Chemistry, 页码：7161-7168 , 文章类型： 研究论文，,卷期：2008年51-22] A series of substituted 2-benzyl-3-aryl-7-trifluoromethylindazoles were prepd. as LXR modulators. These compds. were partial agonists in transactivation assays when compared to T0901317 and were slightly weaker with res... Characterization of Thien-2-yl 1S,2R-Milnacipran Analogues as Potent Norepinephrine/Serotonin Transporter Inhibitors for the Treatment of Neuropathic Pain. [作者：Dyck, Brian;Tamiya, Junko;Jovic, Florence;Pick, Rebecca R.;Bradbury, Margaret J.;O'Brien, Julie;Wen, Jenny;Johns, Michael;Madan, Ajay;Fleck, Beth A.;Foster, Alan C.;Li, Binfeng;Zhang, Mingzhu;Tran, Joe A.;Vickers, Troy;Grey, Jonathan;Saunders, John;Chen,,期刊：Journal of Medicinal Chemistry, 页码：7265-7272 , 文章类型： 研究论文，,卷期：2008年51-22] Thien-2-yl 1S,2R-milnacipran analogs were synthesized and characterized as norepinephrine/serotonin transporter inhibitors. These compds. possessed higher potencies than 1S,2R-milnacipran while maintaining low mol. wt. a... Synthesis and Biological Evaluation of a Series of Liver-Selective Phosphonic Acid Thyroid Hormone Receptor Agonists and Their Prodrugs. [作者：Boyer, Serge H.;Jiang, Hongjian;Jacintho, Jason D.;Reddy, Mali Venkat;Li, Haiqing;Li, Wenyu;Godwin, Jennifer L.;Schulz, William G.;Cable, Edward E.;Hou, Jinzhao;Wu, Rongrong;Fujitaki, James M.;Hecker, Scott J.;Erion, Mark D.;,期刊：Journal of Medicinal Chemistry, 页码：7075-7093 , 文章类型： 研究论文，,卷期：2008年51-22] Phosphonic acid (PA) thyroid hormone receptor (TR) agonists were synthesized to exploit the poor distribution of PA-based drugs to extrahepatic tissues and thereby to improve the therapeutic index. Nine PAs showed excell... Discovery of Boronic Acids as Novel and Potent Inhibitors of Fatty Acid Amide Hydrolase. [作者：Minkkila, Anna;Saario, Susanna M.;Kasnanen, Heikki;Leppanen, Jukka;Poso, Antti;Nevalainen, Tapio;,期刊：Journal of Medicinal Chemistry, 页码：7057-7060 , 文章类型： 研究论文，,卷期：2008年51-22] A series of com. phenyl-, heteroaryl-, alkyl-, and alkenylboronic acids were evaluated for their FAAH and MGL inhibitory activities. The compds. were generally selective for FAAH, with IC50 in the nanomolar or low-micro... Discovery of Ligands for a Novel Target, the Human Telomerase RNA, Based on Flexible-Target Virtual Screening and NMR. [作者：Pinto, Irene Gomez;Guilbert, Christophe;Ulyanov, Nikolai B.;Stearns, Jay;James, Thomas L.;,期刊：Journal of Medicinal Chemistry, 页码：7205-7215 , 文章类型： 研究论文，,卷期：2008年51-22] The human ribonucleoprotein telomerase is a validated anticancer drug target, and hTR-P2b is a part of the human telomerase RNA (hTR) essential for its activity. Interesting ligands that bind hTR-P2b were identified by ... Acylguanidines as Bioisosteres of Guanidines: NG-Acylated Imidazolylpropylguanidines, a New Class of Histamine H2 Receptor Agonists. [作者：Ghorai, Prasanta;Kraus, Anja;Keller, Max;Gotte, Carsten;Igel, Patrick;Schneider, Erich;Schnell, David;Bernhardt, Gunther;Dove, Stefan;Zabel, Manfred;Elz, Sigurd;Seifert, Roland;Buschauer, Armin;,期刊：Journal of Medicinal Chemistry, 页码：7193-7204 , 文章类型： 研究论文，,卷期：2008年51-22] N1-Aryl(heteroaryl)alkyl-N2-[3-(1H-imidazol-4-yl)propyl]guanidines are potent histamine H2-receptor (H2R) agonists, but their applicability is compromised by the lack of oral bioavailability and CNS penetration. To impro... Alteration of the Bis-tetrahydrofuran Core Stereochemistries in Asimicin Can Affect the Cytotoxicity. [作者：Sinha, Subhash C.;Chen, Zhiyong;Huang, Zheng-Zheng;Nakamaru-Ogiso, Eiko;Pietraszkiewicz, Halina;Edelstein, Matthew;Valeriote, Frederick;,期刊：Journal of Medicinal Chemistry, 页码：7045-7048 , 文章类型： 研究论文，,卷期：2008年51-22] A systematic anal. using 10 synthetic asimicin stereoisomers, e.g. I, revealed that the stereochem. of the bis-tetrahydrofuran core, including the THF rings and the adjacent hydroxy functions, had significant effect on i... Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1. [作者：Meng, He;Krishnaji, Subrahmanian Tarakkad;Beinborn, Martin;Kumar, Krishna;,期刊：Journal of Medicinal Chemistry, 页码：7303-7307 , 文章类型： 研究论文，,卷期：2008年51-22] The relative simplicity and high specificity of peptide therapeutics has fueled recent interest. However, peptide and protein drugs generally require injection and suffer from low metabolic stability. We report here th... Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease. [作者：Zhang, Xiaohu;Tellew, John E.;Luo, Zhiyong;Moorjani, Manisha;Lin, Emily;Lanier, Marion C.;Chen, Yongsheng;Williams, John P.;Saunders, John;Lechner, Sandra M.;Markison, Stacy;Joswig, Tanya;Petroski, Robert;Piercey, Jaime;Kargo, William;Malany, Siobhan;Sant,期刊：Journal of Medicinal Chemistry, 页码：7099-7110 , 文章类型： 研究论文，,卷期：2008年51-22] (Heterocyclic Compounds (More Than One Hetero Atom)) Section 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)pyrimidines bearing substituted pyridyl groups as C-6 substituents were prepd. as selective adenosine hA2A receptor a... Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors. [作者：Ramurthy, Savithri;Subramanian, Sharadha;Aikawa, Mina;Amiri, Payman;Costales, Abran;Dove, Jeff;Fong, Susan;Jansen, Johanna M.;Levine, Barry;Ma, Sylvia;McBride, Christopher M.;Michaelian, Jonah;Pick, Teresa;Poon, Daniel J.;Girish, Sandhya;Shafer, Cynthia M,期刊：Journal of Medicinal Chemistry, 页码：7049-7052 , 文章类型： 研究论文，,卷期：2008年51-22] A series of arylaminobenzimidazoles, e.g. I, was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compds. that are potent in vitro and show desirable in v... Bis-pyranobenzoquinones as a New Family of Reversal Agents of the Multidrug Resistance Phenotype Mediated by P-Glycoprotein in Mammalian Cells and the Protozoan Parasite Leishmania. [作者：Jimenez-Alonso, Sandra;Perez-Lomas, Antonio L.;Estevez-Braun, Ana;Martinez, Francisco Munoz;Orellana, Haydee Chavez;Ravelo, Angel G.;Gamarro, Francisco;Castanys, Santiago;Lopez, Matias;,期刊：Journal of Medicinal Chemistry, 页码：7132-7143 , 文章类型： 研究论文，,卷期：2008年51-22] A set of bis-pyranobenzoquinones have been synthesized through a direct and highly efficient approach based on a double intramol. domino Knoevenagel hetero Diels-Alder reaction. These bis-pyranobenzoquinone derivs. are ... Synthesis, Cytotoxic Activity, and Mechanism of Action of Furo[2,3-c]acridin-6-one and Benzo[b]furo[3,2-h]acridin-6-one Analogues of Psorospermin and Acronycine. [作者：Boutefnouchet, Sabrina;Gaboriaud-Kolar, Nicolas;Minh, Nguyen Tuan;Depauw, Sabine;David-Cordonnier, Marie-Helene;Pfeiffer, Bruno;Leonce, Stephane;Pierre, Alain;Tillequin, Francois;Lallemand, Marie-Christine;Michel, Sylvie;,期刊：Journal of Medicinal Chemistry, 页码：7287-7297 , 文章类型： 研究论文，,卷期：2008年51-22] Compds., e.g. I and II, possessing the epoxyfuran system present in the natural cytotoxic dihydrofuroxanthone psorospermin fused onto the acridone or benzo[b]acridone chromophores present in the antitumor acronycine and ...