- Solution Structure of the Supramolecular Adduct between a Liver Cytosolic Bile Acid Binding Protein and a Bile Acid-Based Gadolinium(III)-Chelate, a Potential Hepatospecific Magnetic Resonance Imaging Contrast Agent.
[作者：Tomaselli, Simona;Zanzoni, Serena;Ragona, Laura;Gianolio, Eliana;Aime, Silvio;Assfalg, Michael;Molinari, Henriette;,期刊：Journal of Medicinal Chemistry, 页码：6782-6792 , 文章类型： 研究论文，,卷期：2008年51-21]
- Bile acid-conjugated gadolinium chelates were shown to display promising features for the development of hepatospecific contrast agents for magnetic resonance imaging (MRI). The study of the pharmacokinetics of these co...
- Linking Bisphosphonates to the Free Amino Groups in Fluoroquinolones: Preparation of Osteotropic Prodrugs for the Prevention of Osteomyelitis.
[作者：Houghton, Tom J.;Tanaka, Kelly S. E.;Kang, Ting;Dietrich, Evelyne;Lafontaine, Yanick;Delorme, Daniel;Ferreira, Sandra S.;Viens, Frederic;Arhin, Francis F.;Sarmiento, Ingrid;Lehoux, Dario;Fadhil, Ibtihal;Laquerre, Karine;Liu, Jing;Ostiguy, Valerie;Poirier,,期刊：Journal of Medicinal Chemistry, 页码：6955-6969 , 文章类型： 研究论文，,卷期：2008年51-21]
- Osteomyelitis is an infection located in bone and a notoriously difficult disease to manage, requiring frequent and heavy doses of systemically administered antibiotics. Targeting antibiotics to the bone after systemic ...
- Antibody Conjugates of 7-Ethyl-10-hydroxycamptothecin (SN-38) for Targeted Cancer Chemotherapy.
[作者：Moon, Sung-Ju;Govindan, Serengulam V.;Cardillo, Thomas M.;D'Souza, Christopher A.;Hansen, Hans J.;Goldenberg, David M.;,期刊：Journal of Medicinal Chemistry, 页码：6916-6926 , 文章类型： 研究论文，,卷期：2008年51-21]
- CPT-11 is a clin. used cancer drug, and it is a prodrug of the potent topoisomerase I inhibitor, SN-38 (7-ethyl-10-hydroxycamptothecin, I). To bypass the need for the in vivo conversion of CPT-11 and increase the therape...
- Advances toward New Antidepressants with Dual Serotonin Transporter and 5-HT1A Receptor Affinity within a Class of 3-Aminochroman Derivatives. Part 2.
[作者：Hatzenbuhler, Nicole T.;Baudy, Reinhardt;Evrard, Deborah A.;Failli, Amedeo;Harrison, Boyd L.;Lenicek, Steven;Mewshaw, Richard E.;Saab, Annmarie;Shah, Uresh;Sze, Jean;Zhang, Minsheng;Zhou, Dahui;Chlenov, Michael;Kagan, Michael;Golembieski, Jeannette;Hornby,期刊：Journal of Medicinal Chemistry, 页码：6980-7004 , 文章类型： 研究论文，,卷期：2008年51-21]
- (Heterocyclic Compounds (One Hetero Atom)) Section Novel compds. combining a 5-HT1A moiety (3-aminochroman scaffold) and a 5-HT transporter (indole analogs) linked through a common basic nitrogen via an alkyl chain attac...
- Improved synthesis of 6-epi-dictyostatin and antitumor efficacy in mice bearing MDA-MB231 human breast cancer xenografts.
[作者：Eiseman, Julie L.;Bai, Lihua;Jung, Won-Hyuk;Moura-Letts, Gustavo;Day, Billy W.;Curran, Dennis P.;,期刊：Journal of Medicinal Chemistry, 页码：6650-6653 , 文章类型： 研究论文，,卷期：2008年51-21]
- Structure-activity studies centered on the naturally occurring antitumor agent dictyostatin have recently identified several highly active epimers and analogs. From these compds., 6-epi-dictyostatin was selected for sca...
- Molecular Probes for Imaging Myelinated White Matter in CNS.
[作者：Wu, Chunying;Wei, Jinjun;Tian, Donghua;Feng, Yue;Miller, Robert H.;Wang, Yanming;,期刊：Journal of Medicinal Chemistry, 页码：6682-6688 , 文章类型： 研究论文，,卷期：2008年51-21]
- Abnormalities and changes in myelination in the brain are seen in many neurodegenerative disorders such as multiple sclerosis (MS). Direct detection and quantification of myelin content in vivo is desired to facilitate ...
- Prevention of Drug-Induced Memory Impairment by Immunopharmacotherapy.
[作者：Treweek, Jennifer B.;Sun, Chengzao;Mayorov, Alexander V.;Qi, Longwu;Levy, Coree L.;Roberts, Amanda J.;Dickerson, Tobin J.;Janda, Kim D.;,期刊：Journal of Medicinal Chemistry, 页码：6866-6875 , 文章类型： 研究论文，,卷期：2008年51-21]
- One approach to treating drug abuse uses antidrug antibodies to immunize subjects against the illicit substance rather than administering therapeutics that target the specific CNS site of action. At present, passive vacc...
- Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications.
[作者：Li, Jie Jack;Iula, Donna M.;Nguyen, Maria N.;Hu, Lain-Yen;Dettling, Danielle;Johnson, Theodore R.;Du, Daniel Y.;Shanmugasundaram, Veerabahu;Van Camp, Jennifer A.;Wang, Zhi;Harter, William G.;Yue, Wen-Song;Boys, Mark L.;Wade, Kimberly J.;Drummond, Elena M.,期刊：Journal of Medicinal Chemistry, 页码：7010-7014 , 文章类型： 研究论文，,卷期：2008年51-21]
- 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile [PF-0998425, (I)] is a novel, nonsteroidal androgen receptor antagonist for sebum control and treatment of androgenetic alopecia. It is potent, selective, a...
- Discovery of Substituted 4-(Pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as Potent and Highly Selective Rho Kinase (ROCK-II) Inhibitors.
[作者：Feng, Yangbo;Yin, Yan;Weiser, Amiee;Griffin, Evelyn;Cameron, Michael D.;Lin, Li;Ruiz, Claudia;Schurer, Stephan C.;Inoue, Toshihiro;Rao, P. Vasanth;Schroter, Thomas;LoGrasso, Philip;,期刊：Journal of Medicinal Chemistry, 页码：6642-6645 , 文章类型： 研究论文，,卷期：2008年51-21]
- The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compd. SR-3677 (I) had an IC50 of ~3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinas...
- Hit Identification and Binding Mode Predictions by Rigorous Free Energy Simulations.
[作者：Michel, Julien;Essex, Jonathan W.;,期刊：Journal of Medicinal Chemistry, 页码：6654-6664 , 文章类型： 研究论文，,卷期：2008年51-21]
- The identification of lead mols. using computational modeling often relies on approx., high-throughput approaches, of limited accuracy. The authors show here that, with a methodol. the authors recently developed, it is p...
- Novel D3 Selective Dopaminergics Incorporating Enyne Units as Nonaromatic Catechol Bioisosteres: Synthesis, Bioactivity, and Mutagenesis Studies.
[作者：Doerfler, Miriam;Tschammer, Nuska;Hamperl, Katharina;Huebner, Harald;Gmeiner, Peter;,期刊：Journal of Medicinal Chemistry, 页码：6829-6838 , 文章类型： 研究论文，,卷期：2008年51-21]
- Enynes of type 4 and 5 as long chain derivs. of the nonarom. dopamine D3 receptor agonist 3 (FAUC 73) were prepd. by exploiting chemoselective functionalization of the azido-substituted vinyl triflate 9. Radioligand bind...
- Quantitative Structure-Activity Relationship and Complex Network Approach to Monoamine Oxidase A and B Inhibitors.
[作者：Santana, Lourdes;Gonzalez-Diaz, Humberto;Quezada, Elias;Uriarte, Eugenio;Yanez, Matilde;Vina, Dolores;Orallo, Francisco;,期刊：Journal of Medicinal Chemistry, 页码：6740-6751 , 文章类型： 研究论文，,卷期：2008年51-21]
- The work provides a new model for the prediction of the MAO-A and -B inhibitor activity by the use of combined complex networks and QSAR methodologies. On the basis of the obtained model, the authors prepd. and assayed ...
- Structure-Based Virtual Screening and Biological Evaluation of Mycobacterium tuberculosis Adenosine 5'-Phosphosulfate Reductase Inhibitors.
[作者：Cosconati, Sandro;Hong, Jiyoung A.;Novellino, Ettore;Carroll, Kate S.;Goodsell, David S.;Olson, Arthur J.;,期刊：Journal of Medicinal Chemistry, 页码：6627-6630 , 文章类型： 研究论文，,卷期：2008年51-21]
- Tuberculosis is among the world's deadliest infectious diseases. APS reductase catalyzes the first committed step in bacterial sulfate redn. and is a validated drug target against latent tuberculosis infection. We perf...
- Potential Modes of Interaction of 9-Aminomethyl-9,10-dihydroanthracene (AMDA) Derivatives with the 5-HT2A Receptor: A Ligand Structure-Affinity Relationship, Receptor Mutagenesis and Receptor Modeling Investigation.
[作者：Runyon, Scott P.;Mosier, Philip D.;Roth, Bryan L.;Glennon, Richard A.;Westkaemper, Richard B.;,期刊：Journal of Medicinal Chemistry, 页码：6808-6828 , 文章类型： 研究论文，,卷期：2008年51-21]
- The effects of 3-position substitution of 9-aminomethyl-9,10-dihydroanthracene (AMDA) on 5-HT2A receptor affinity were detd. and compared to a parallel series of DOB-like 1-(2,5-dimethoxyphenyl)-2-aminopropanes substitut...
- Synthesis, In Vitro, and In Silico Evaluation of Organometallic Technetium and Rhenium Thymidine Complexes with Retained Substrate Activity toward Human Thymidine Kinase Type 1.
[作者：Desbouis, Dominique;Struthers, Harriet;Spiwok, Vojtech;Kuster, Tatiana;Schibli, Roger;,期刊：Journal of Medicinal Chemistry, 页码：6689-6698 , 文章类型： 研究论文，,卷期：2008年51-21]
- Human cytosolic thymidine kinase (hTK1) proved to be a suitable target for noninvasive imaging of cancer cell proliferation using radiolabeled substrates such as [18F]fluorothymidine ([18F]FLT). However, a based on the ...
- Semisynthetic Cyclopamine Analogues as Potent and Orally Bioavailable Hedgehog Pathway Antagonists.
[作者：Tremblay, Martin R.;Nevalainen, Marta;Nair, Somarajan J.;Porter, James R.;Castro, Alfredo C.;Behnke, Mark L.;Yu, Lin-Chen;Hagel, Margit;White, Kerry;Faia, Kerrie;Grenier, Louis;Campbell, Matthew J.;Cushing, Jill;Woodward, Caroline N.;Hoyt, Jennifer;Foley,,期刊：Journal of Medicinal Chemistry, 页码：6646-6649 , 文章类型： 研究论文，,卷期：2008年51-21]
- antagonists derived from cyclopamine. The acid sensitive D-ring of cyclopamine was homologated utilizing a sequence of chemoselective cyclopropanation and stereoselective acid-catalyzed rearrangement. Further modificati...
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