- Inhibition of the Signal Transducer and Activator of Transcription-3 (STAT3) Signaling Pathway by 4-Oxo-1-Phenyl-1,4-Dihydroquinoline-3-Carboxylic Acid Esters.
[作者:Xu, Jun;Cole, Derek C.;Chang, Chao-Pei Betty;Ayyad, Ramzi;Asselin, Magda;Hao, Wenshan;Gibbons, James;Jelinsky, Scott A.;Saraf, Kathryn A.;Park, Kaapjoo;,期刊:Journal of Medicinal Chemistry, 页码:4115-4121 , 文章类型: 研究论文,,卷期:2008年51-14]
- The JAK-STAT3 pathway regulates genes that are important in cell proliferation and thus is a promising target for cancer therapy. A high-throughput screening (HTS) campaign using an Apo-ONE Homogenous Caspase 3/7 assay ...
- Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]- 2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxa mide (MK-0731) for the Treatment of Taxane-Refractory C
[作者:Cox, Christopher D.;Coleman, Paul J.;Breslin, Michael J.;Whitman, David B.;Garbaccio, Robert M.;Fraley, Mark E.;Buser, Carolyn A.;Walsh, Eileen S.;Hamilton, Kelly;Schaber, Michael D.;Lobell, Robert B.;Tao, Weikang;Davide, Joseph P.;Diehl, Ronald E.;Abrams,期刊:Journal of Medicinal Chemistry, 页码:4239-4252 , 文章类型: 研究论文,,卷期:2008年51-14]
- Inhibition of kinesin spindle protein (KSP) is a novel mechanism for treatment of cancer with the potential to overcome limitations assocd. with currently employed cytotoxic agents. Herein, we describe a C2-hydroxymethy...
- Complexation of the anti-Trypanosoma cruzi Drug Benznidazole Improves Solubility and Efficacy.
[作者:Nogueira Silva, Jean Jerley;Pavanelli, Wander Rogerio;Salazar Gutierrez, Fredy R.;Alves Lima, Francisco Chagas;Ferreira da Silva, Alberico Borges;Santana Silva, Joao;Wagner Franco, Douglas;,期刊:Journal of Medicinal Chemistry, 页码:4104-4114 , 文章类型: 研究论文,,卷期:2008年51-14]
- The ruthenium complex, trans-[Ru(Bz)(NH3)4SO2](CF3SO3)2 (1), Bz = benznidazole (N-benzyl-2-(2-nitro-1H-imidazol-1-yl)acetamide), is more hydrosol. and more active (IC50try/1 h = 79 ?3 mM) than free benznidazole (2) (IC50...
- Discovery of Phosphonic Diamide Prodrugs and Their Use for the Oral Delivery of a Series of Fructose 1,6-Bisphosphatase Inhibitors.
[作者:Dang, Qun;Kasibhatla, Srinivas Rao;Jiang, Tao;Fan, Kevin;Liu, Yan;Taplin, Frank;Schulz, William;Cashion, Daniel K.;Reddy, K. Raja;van Poelje, Paul D.;Fujitaki, James M.;Potter, Scott C.;Erion, Mark D.;,期刊:Journal of Medicinal Chemistry, 页码:4331-4339 , 文章类型: 研究论文,,卷期:2008年51-14]
- Like most phosphonic acids, the recently discovered potent and selective thiazole phosphonic acid inhibitors of fructose 1,6-bisphosphatase (FBPase) exhibited low oral bioavailability (OBAV) and therefore required a prod...
- N-Hydroxypyrazolyl glycine derivatives as selective N-methyl-D-aspartic acid receptor ligands.
[作者:Clausen, Rasmus P.;Christensen, Caspar;Hansen, Kasper B.;Greenwood, Jeremy R.;Jorgensen, Lars;Micale, Nicola;Madsen, Jens Christian;Nielsen, Birgitte;Egebjerg, Jan;Brauner-Osborne, Hans;Traynelis, Stephen F.;Kristensen, Jesper L.;,期刊:Journal of Medicinal Chemistry, 页码:4179-4187 , 文章类型: 研究论文,,卷期:2008年51-14]
- A series of analogs based on N-hydroxypyrazole as a bioisostere for the distal carboxylate group of aspartate have been designed, synthesized, and pharmacol. characterized. Affinity studies on the major glutamate recept...
- Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogs: New insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
[作者:Sagot, Emanuelle;Pickering, Darryl S.;Pu, Xiaosui;Umberti, Michelle;Stensboel, Tine B.;Nielsen, Birgitte;Chapelet, Marion;Bolte, Jean;Gefflaut, Thierry;Bunch, Lennart;,期刊:Journal of Medicinal Chemistry, 页码:4093-4103 , 文章类型: 研究论文,,卷期:2008年51-14]
- (S)-Glutamic acid (Glu) is the major excitatory neurotransmitter in the central nervous system (CNS) activating the plethora of ionotropic Glu receptors (iGluRs) and metabotropic Glu receptors (mGluRs). In this paper, w...
- Turning Low-Molecular-Weight Drugs into Prolonged Acting Prodrugs by Reversible Pegylation: A Study with Gentamicin.
[作者:Marcus, Yonit;Sasson, Keren;Fridkin, Mati;Shechter, Yoram;,期刊:Journal of Medicinal Chemistry, 页码:4300-4305 , 文章类型: 研究论文,,卷期:2008年51-14]
- Pegylation is a powerful technol. to prolong the action of proteins in vivo, but it is impractical for low-mol.-wt. (LMW) drugs, which are usually inactivated upon such modification. Here, we have applied a recently dev...
- Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedi oic acid: A novel selective inhibitor of human excitatory amino acid transporter subtype 2.
[作者:Sagot, Emanuelle;Jensen, Anders A.;Pickering, Darryl S.;Pu, Xiaosui;Umberti, Michelle;Stensboel, Tine B.;Nielsen, Birgitte;Assaf, Zeinab;Aboab, Betina;Bolte, Jean;Gefflaut, Thierry;Bunch, Lennart;,期刊:Journal of Medicinal Chemistry, 页码:4085-4092 , 文章类型: 研究论文,,卷期:2008年51-14]
- In the mammalian central nervous system (CNS), the action of sodium dependent excitatory amino acid transporters (EAATs) is responsible for termination of glutamatergic neurotransmission by reuptake of (S)-glutamate (Glu...
- Discovery of Nonsteroidal 17b-Hydroxysteroid Dehydrogenase 1 Inhibitors by Pharmacophore-Based Screening of Virtual Compound Libraries.
[作者:Schuster, Daniela;Nashev, Lyubomir G.;Kirchmair, Johannes;Laggner, Christian;Wolber, Gerhard;Langer, Thierry;Odermatt, Alex;,期刊:Journal of Medicinal Chemistry, 页码:4188-4199 , 文章类型: 研究论文,,卷期:2008年51-14]
- 17b-Hydroxysteroid dehydrogenase type 1 (17b-HSD1) plays a pivotal role in the local synthesis of the most potent estrogen estradiol. Its expression is a prognostic marker for the outcome of patients with breast cancer ...
- Synthesis and Pharmacological Evaluation of Novel g-Aminobutyric Acid Type B (GABAB) Receptor Agonists as Gastroesophageal Reflux Inhibitors.
[作者:Alstermark, Christer;Amin, Kosrat;Dinn, Sean R.;Elebring, Thomas;Fjellstroem, Ola;Fitzpatrick, Kevin;Geiss, William B.;Gottfries, Johan;Guzzo, Peter R.;Harding, James P.;Holmen, Anders;Kothare, Mohit;Lehmann, Anders;Mattsson, Jan P.;Nilsson, Karolina;Sund,期刊:Journal of Medicinal Chemistry, 页码:4315-4320 , 文章类型: 研究论文,,卷期:2008年51-14]
- agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the most important mechanism for gastroesophageal reflux. Thus, GABAB agonists could be exploited for the treatment of gastroesophagea...
- Carbamoylphosphonate matrix metalloproteinase inhibitors: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor-synthesis and pharmacodynamic and pharmacokinetic analysis. [Errat
[作者:Hoffman, Amnon;Qadri, Bashir;Frant, Julia;Katz, Yiffat;Bhusare, Sudhakar R.;Breuer, Eli;Hadar, Rivka;Reich, Reuven;,期刊:Journal of Medicinal Chemistry, 页码:4357-4358 , 文章类型: 研究论文,,卷期:2008年51-14]
- version of the paragraph is given.
- Discovery of alogliptin: A potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. [Erratum to document cited in CA147:045193].
[作者:Feng, Jun;Zhang, Zhiyuan;Wallace, Michael B.;Stafford, Jeffrey A.;Kaldor, Stephen W.;Kassel, Daniel B.;Navre, Marc;Shi, Lihong;Skene, Robert J.;Asakawa, Tomoko;Takeuchi, Koji;Xu, Rongda;Webb, David R.;Gwaltney, Stephen L.;,期刊:Journal of Medicinal Chemistry, 页码:4357-4357 , 文章类型: 研究论文,,卷期:2008年51-14]
- On page 2297, Figure 1 is incorrect; the correct version of the figure is given. On page 2298, Figure 4 is incorrect; the correct version of the figure is given.
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