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Kinds of Potent Terms modified by Potent Selected AbstractsAnti-tumor efficacy of the nucleoside analog 1-(2-deoxy-2-fluoro-4-thio-,-D-arabinofuranosyl) cytosine (4,-thio-FAC) in human pancreatic and ovarian tumor xenograft modelsINTERNATIONAL JOURNAL OF CANCER, Issue 6 2005Deborah A. Zajchowski Abstract 1-(2-Deoxy-2-fluoro-4-thio-,- D -arabinofuranosyl) cytosine (4,-thio-FAC) is a deoxycytidine analog that has been shown previously to have impressive anti-proliferative and cytotoxic effects in vitro and in vivo toward colorectal and gastric tumors. In our present studies, the pharmacokinetic behavior in nude mice and the effectiveness of 4,-thio-FAC against human pancreatic and ovarian tumor growth were assessed in comparison with standard chemotherapeutic agents. Potent in vitro anti-proliferative effects were observed against pancreatic (Capan-1, MIA-PaCa-2, BxPC-3) and ovarian (SK-OV-3, OVCAR-3, ES-2) cancer cell lines with IC50 of 0.01,0.2 ,M. In vivo anti-tumor activity was evaluated in nude mice bearing subcutaneously (s.c.) implanted human pancreatic tumor xenografts or intraperitoneally (i.p.) disseminated human ovarian xenografted tumors. Oral daily administration of 4,-thio-FAC for 8,10 days significantly inhibited the growth of gemcitabine-resistant BxPC-3 pancreatic tumors and induced regression of gemcitabine-refractory Capan-1 tumors. 4,-Thio-FAC was also a highly effective inhibitor of ovarian peritoneal carcinomatosis. In the SK-OV-3 and ES-2 ovarian cancer models, 4,-thio-FAC prolonged survival to a greater extent than that observed with gemcitabine. Furthermore, the superiority of 4,-thio-FAC to carboplatin and paclitaxel was demonstrated in the ES-2 clear cell ovarian carcinoma model. Studies provide evidence that 4,-thio-FAC is a promising new alternative to gemcitabine and other chemotherapeutic drugs in the treatment of a variety of tumor indications, including pancreatic and ovarian carcinoma. © 2004 Wiley-Liss, Inc. [source] Identification of Thiazolidinones Spiro-Fused to Indolin-2-ones as Potent and Selective Inhibitors of the Mycobacterium tuberculosis Protein Tyrosine Phosphatase,B,ANGEWANDTE CHEMIE, Issue 34 2010Viktor Das beste aus 40,000: Detaillierte Untersuchungen zur Struktur-Aktivitäts-Beziehung enthüllten Schlüsselstrukturelemente von Indolin-2-on-3-spirothiazolidinonen (siehe Beispiel) und deren für eine starke Inhibierung des pathophysiologisch wichtigen Titelproteins geeignete Konfiguration. [source] Lipophilic Pyridinium Bisphosphonates: Potent ,, T Cell Stimulators,ANGEWANDTE CHEMIE, Issue 6 2010Yonghui Zhang Dr. Mit langen Alkylketten versehene, lipophile Pyridiniumbisphosphonate (siehe Bild: P,rot, N,blau, C,orange, H,grau) stimulieren humane ,,-T-Zellen, die den V,2V,2-T-Zellrezeptor exprimieren. Ihre Wirkung ist stärker als diejenige von Zoledronat, das gegen Brust- und Prostatakrebs aktiv ist. Die lipophilen Bisphosphonate binden nur schwach in Knochen, sodass Nebenwirkungen, wie sie sonst bei der klinischen Verwendung von Bisphosphonaten auftreten, weniger wahrscheinlich sind. [source] Design and Synthesis of Highly Potent and Plasma-Stable Dimeric Inhibitors of the PSD-95,NMDA Receptor Interaction,ANGEWANDTE CHEMIE, Issue 51 2009Anders Bach Dr. Im Doppel: Die Dimerisierung monomerer Peptidliganden für die PDZ-Domänen des Proteins PSD-95 (postsynaptische Dichte,95) liefert leistungsfähige Inhibitoren von Protein-Protein-Wechselwirkungen, die in Blutplasma stabil sind. Durch Optimierung der Länge des Polyethylenglycol-Linkers gelangt man zu Inhibitoren der PDZ1-2-Domäne (siehe Bild) mit bislang unerreichter Affinität. [source] Thirdhand Smoke Identified as Potent, Enduring CarcinogenCA: A CANCER JOURNAL FOR CLINICIANS, Issue 4 2010John Henry Dreyfuss No abstract is available for this article. [source] Exploring QSAR for Substituted 2-Sulfonyl-Phenyl-Indol Derivatives as Potent and Selective COX-2 Inhibitors Using Different Chemometrics ToolsCHEMICAL BIOLOGY & DRUG DESIGN, Issue 6 2008Mehdi Khoshneviszadeh Selective inhibition of cyclooxygenase-2 inhibitors is an important strategy in designing of potent anti-inflammatory compounds with significantly reduced side effects. The present quantitative structure,activity relationship study, attempts to explore the structural and physicochemical requirements of 2-sulfonyl,phenyl,indol derivatives (n = 30) for COX-2 inhibitory activity using chemical, topological, geometrical, and quantum descriptors. Some statistical techniques like stepwise regression, multiple linear regression with factor analysis as the data preprocessing (FA-MLR), principal component regression analysis, and genetic algorithms partial least squares analysis were applied to derive the quantitative structure,activity relationship models. The generated equations were statistically validated using cross-validation and external test set. The quality of equations obtained from stepwise multiple linear regression, FA-MLR, principal component regression analysis and PLS were in the acceptable statistical range. The best multiple linear regression equation obtained from factor analysis (FA-MLR) as the preprocessing step could predict 77.5% of the variance of the cyclooxygenase-2 inhibitory activity whereas that derived from genetic algorithms partial least squares could predict 84.2% of variances. The results of quantitative structure,activity relationship models suggested the importance of lipophilicity, electronegativity, molecular area and steric parameters on the cyclooxygenase-2 inhibitory activity. [source] ChemInform Abstract: An Efficient Asymmetric Synthesis of the Potent ,-Blocker ICI-118,551 Allows the Determination of Enantiomer Dependency on Biological Activity.CHEMINFORM, Issue 43 2010James R. Baker Abstract A highly efficient asymmetric synthesis of the title compound is developed. [source] ChemInform Abstract: Discovery of 5-Substituted 2-Amino-4-chloro-8-( (4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7,8-dihydropteridin-6 (5H)-ones as Potent and Selective Hsp90 Inhibitors.CHEMINFORM, Issue 40 2009Xiaoyuan Li Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Discovery of Novel Acetanilide Derivatives as Potent and Selective ,3-Adrenergic Receptor Agonists.CHEMINFORM, Issue 36 2009Tatsuya Maruyama Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Potent and Selective Inhibitors of Helicobacter pylori glutamate Racemase (MurI): Pyridodiazepine Amines.CHEMINFORM, Issue 26 2009Bolin Geng Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Discovery of Potent, Selective Sulfonylfuran Urea Endothelial Lipase Inhibitors.CHEMINFORM, Issue 20 2009Krista B. Goodman Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: Chlorahololides C,F: A New Class of Potent and Selective Potassium Channel Blockers from Chloranthus holostegius.CHEMINFORM, Issue 37 2008Sheng-Ping Yang Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] ChemInform Abstract: The Discovery of GSK221149A: A Potent and Selective Oxytocin Antagonist.CHEMINFORM, Issue 26 2008John Liddle Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Potent, Selective, and Orally Active Adenosine A2A Receptor Antagonists: Arylpiperazine Derivatives of Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.CHEMINFORM, Issue 29 2007Bernard R. Neustadt Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Identification of a Novel 3,5-Disubstituted Pyridine as a Potent, Selective, and Orally Active Inhibitor of Akt1 Kinase.CHEMINFORM, Issue 42 2006Sheela A. Thomas Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis of Pyrazoles and Isoxazoles as Potent ,v,3 Receptor Antagonists.CHEMINFORM, Issue 37 2006Thomas D. Penning Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Hit-to-Lead Studies: The Discovery of Potent, Orally Bioavailable Thiazolopyrimidine CXCR2 Receptor Antagonists.CHEMINFORM, Issue 21 2006Andrew Baxter Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Discovery of a Substituted 8-Arylquinoline Series of PDE4 Inhibitors: Structure,Activity Relationship, Optimization, and Identification of a Highly Potent, Well Tolerated, PDE4 Inhibitor.CHEMINFORM, Issue 9 2006Dwight Macdonald Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] 2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine Analogues: Highly Potent, Orally Active, Adenosine A2A Antagonists.CHEMINFORM, Issue 4 2006Part 1. Abstract For Abstract see ChemInform Abstract in Full Text. [source] Structure-Based Design of Potent and Selective Inhibitors of Collagenase-3 (MMP-13).CHEMINFORM, Issue 26 2005Soong-Hoon Kim Abstract For Abstract see ChemInform Abstract in Full Text. [source] 3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: A Novel Class of Potent, Selective Cyclooxygenase-2 (COX-2) Inhibitors.CHEMINFORM, Issue 16 2005Ramani R. Ranatunge Abstract For Abstract see ChemInform Abstract in Full Text. [source] Design and Synthesis of 1-(4-Benzoylphenyl)imidazole Derivatives as New Potent 20-HETE Synthase Inhibitors.CHEMINFORM, Issue 9 2005Toshio Nakamura Abstract For Abstract see ChemInform Abstract in Full Text. [source] Potent and Selective Proline Derived Dipeptidyl Peptidase IV Inhibitors.CHEMINFORM, Issue 5 2005Scott D. Edmondson No abstract is available for this article. [source] Discovery of Potent and Orally Bioavailable N,N,-Diarylurea Antagonists for the CXCR2 Chemokine Receptor.CHEMINFORM, Issue 48 2004Qi Jin Abstract For Abstract see ChemInform Abstract in Full Text. [source] Imidazo[1,2-b]pyridazines: A Potent and Selective Class of Cyclin-Dependent Kinase Inhibitors.CHEMINFORM, Issue 35 2004Andrew P. Thomas Abstract For Abstract see ChemInform Abstract in Full Text. [source] (S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo [1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide Is a Potent and Efficacious KCNQ2 Opener which Inhibits Induced Hyperexcitability of Rat Hippocampal Neurons.CHEMINFORM, Issue 31 2004Yong-Jin Wu Abstract For Abstract see ChemInform Abstract in Full Text. [source] Potent and Selective Inhibitors of Bacterial Methionyl tRNA Synthetase Derived from an Oxazolone,Dipeptide ScaffoldCHEMINFORM, Issue 31 2004Manish Tandon Abstract For Abstract see ChemInform Abstract in Full Text. [source] Quinolines as Extremely Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile Dysfunction.CHEMINFORM, Issue 30 2004Yingzhi Bi Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis of Cinnamic Acids and Related Isosteres as Potent and Selective ,v,3 Receptor Antagonists.CHEMINFORM, Issue 29 2004Thomas D. Penning Abstract For Abstract see ChemInform Abstract in Full Text. [source] Design, Synthesis and Biological Activity of Novel Dimethyl-{2-[6-substituted-indol-1-yl]-ethyl}-amine as Potent, Selective, and Orally-Bioavailable 5-HT1D Agonists.CHEMINFORM, Issue 12 2004Methvin Isaac Abstract For Abstract see ChemInform Abstract in Full Text. [source] |