- Synthesis and Evaluation of [N-methyl-11C]N-Desmethyl-loperamide as a New and Improved PET Radiotracer for Imaging P-gp Function.
[作者:Lazarova, Neva;Zoghbi, Sami S.;Hong, Jinsoo;Seneca, Nicholas;Tuan, Ed;Gladding, Robert L.;Liow, Jeih-San;Taku, Andrew;Innis, Robert B.;Pike, Victor W.;,期刊:Journal of Medicinal Chemistry, 页码:6034-6043 , 文章类型: 研究论文,,卷期:2008年51-19]
- [11C]Loperamide has been proposed for imaging P-glycoprotein (P-gp) function with positron emission tomog. (PET), but its metab. to [N-methyl-11C]N-desmethyl-loperamide ([11C]dLop; [11C]3) precludes quantification. We c...
- Glycol Porphyrin Derivatives as Potent Photodynamic Inducers of Apoptosis in Tumor Cells.
[作者:Kralova, Jarmila;Briza, Tomas;Moserova, Irena;Dolensky, Bohumil;Vasek, Petr;Pouckova, Pavla;Kejik, Zdenek;Kaplanek, Robert;Martasek, Pavel;Dvorak, Michal;Kral, Vladimir;,期刊:Journal of Medicinal Chemistry, 页码:5964-5973 , 文章类型: 研究论文,,卷期:2008年51-19]
- The design and synthesis of glycol-functionalized porphyrins that contain one to four low mol. wt. glycol chains that are linked via ether bonds to the meta-Ph positions of meso-tetraphenylporphyrin and the comparison of...
- Synthesis, Binding Affinity, and Molecular Docking Analysis of New Benzofuranone Derivatives as Potential Antipsychotics.
[作者:Aranda, Reyes;Villalba, Karen;Ravina, Enrique;Masaguer, Christian F.;Brea, Jose;Areias, Filipe;Dominguez, Eduardo;Selent, Jana;Lopez, Laura;Sanz, Ferran;Pastor, Manuel;Loza, Maria I.;,期刊:Journal of Medicinal Chemistry, 页码:6085-6094 , 文章类型: 研究论文,,卷期:2008年51-19]
- The complex etiol. of schizophrenia has prompted researchers to develop clozapine-related multitarget strategies to combat its symptoms. Here we describe a series of new 6-aminomethylbenzofuranones in an effort to find ...
- Novel A-Ring and B-Ring Modified Combretastatin A-4 (CA-4) Analogues Endowed with Interesting Cytotoxic Activity.
[作者:Simoni, Daniele;Romagnoli, Romeo;Baruchello, Riccardo;Rondanin, Riccardo;Grisolia, Giuseppina;Eleopra, Marco;Rizzi, Michele;Tolomeo, Manlio;Giannini, Giuseppe;Aloatti, Domenico;Castorina, Massimo;Marcellini, Marcella;Pisano, Claudio;,期刊:Journal of Medicinal Chemistry, 页码:6211-6215 , 文章类型: 研究论文,,卷期:2008年51-19]
- A novel class of combretastatins, modified at A-ring or both A- and B-rings, mainly by replacement with benzofuran or benzo[b]thiophene, were synthesized. The new heterocombretastatins showed good cytotoxic activity on ...
- Identification of BRAF Inhibitors through In Silico Screening.
[作者:Luo, Cheng;Xie, Peng;Marmorstein, Ronen;,期刊:Journal of Medicinal Chemistry, 页码:6121-6127 , 文章类型: 研究论文,,卷期:2008年51-19]
- The BRAF protein kinase, a mol. in the RAS-RAF-MEK-ERK signaling pathway, is mutated to harbor elevated kinase activity in ~7% of human cancers, which makes it an important therapeutic target for inhibition. Several BRAF...
- Hydration of Drug-DNA Complexes: Greater Water Uptake for Adriamycin Compared to Daunomycin.
[作者:Yu, Haijia;Ren, Jinsong;Chaires, Jonathan B.;Qu, Xiaogang;,期刊:Journal of Medicinal Chemistry, 页码:5909-5911 , 文章类型: 研究论文,,卷期:2008年51-19]
- binding sites can modulate drug binding to DNA or protein. The authors report here that anthracycline antitumor antibiotics, adriamycin (AM) and daunomycin (DM), binding to DNA is accompanied by different hydration chan...
- Multiple and Single Binding Modes of Fragment-Like Kinase Inhibitors Revealed by Molecular Modeling, Residue Type-Selective Protonation, and Nuclear Overhauser Effects.
[作者:Constantine, Keith L.;Mueller, Luciano;Metzler, William J.;McDonnell, Patricia A.;Todderud, Gordon;Goldfarb, Valentina;Fan, Yi;Newitt, John A.;Kiefer, Susan E.;Gao, Mian;Tortolani, David;Vaccaro, Wayne;Tokarski, John;,期刊:Journal of Medicinal Chemistry, 页码:6225-6229 , 文章类型: 研究论文,,卷期:2008年51-19]
- protein kinase 2 (MK2) include 5-hydroxyisoquinoline (IC50 ~ 85 mM). Modeling studies identified four possible binding modes for this compd. Two-dimensional 1H-1H NOESY data obtained with selectively protonated samples ...
- Design, Synthesis, and Evaluation of Potent and Selective Ligands for the Dopamine 3 (D3) Receptor with a Novel in Vivo Behavioral Profile.
[作者:Chen, Jianyong;Collins, Gregory T.;Zhang, Jian;Yang, Chao-Yie;Levant, Beth;Woods, James;Wang, Shaomeng;,期刊:Journal of Medicinal Chemistry, 页码:5905-5908 , 文章类型: 研究论文,,卷期:2008年51-19]
- receptor. Compd. 12 (I) has a Ki value of 0.41 nM to D3 and a selectivity of >30000- and 800-fold over the D1-like and D2 receptors, resp. Our in vivo functional assays showed that this compd. is a partial agonist at t...
- Novel Microtubule-Interacting Phenoxy Pyridine and Phenyl Sulfanyl Pyridine Analogues for Cancer Therapy.
[作者:Anchoori, Ravi Kumar;Quirine Kortenhorst, Madeleine Susanne;Hidalgo, Manuel;Sarkar, Taradas;Hallur, Gurulingappa;Bai, Ruoli;Van Diest, Paul J.;Hamel, Ernest;Khan, Saeed R.;,期刊:Journal of Medicinal Chemistry, 页码:5953-5957 , 文章类型: 研究论文,,卷期:2008年51-19]
- Current microtubule inhibitory agents used in the clinic to treat cancer have severe side effects, and development of resistance is frequent. We have evaluated the antitumor effect of a novel 30-compd. library of phenoxy...
- Structural Requirements for Drug Inhibition of the Liver Specific Human Organic Cation Transport Protein.
[作者:Ahlin, Gustav;Karlsson, Johan;Pedersen, Jenny M.;Gustavsson, Lena;Larsson, Rolf;Matsson, Paer;Norinder, Ulf;Bergstroem, Christel A. S.;Artursson, Per;,期刊:Journal of Medicinal Chemistry, 页码:5932-5942 , 文章类型: 研究论文,,卷期:2008年51-19]
- transports several cationic drugs including the antidiabetic drug metformin and the anticancer agents oxaliplatin and imatinib. In this study, the authors explored the chem. space of registered oral drugs with the aim o...
- Identification, Characterization and Initial Hit-to-Lead Optimization of a Series of 4-Arylamino-3-Pyridinecarbonitrile as Protein Kinase C theta (PKCq) Inhibitors.
[作者:Cole, Derek C.;Asselin, Magda;Brennan, Agnes;Czerwinski, Robert;Ellingboe, John W.;Fitz, Lori;Greco, Rita;Huang, Xinyi;Joseph-McCarthy, Diane;Kelly, Michael F.;Kirisits, Matthew;Lee, Julie;Li, Yuanhong;Morgan, Paul;Stock, Joseph R.;Tsao, Desiree H. H.;Wis,期刊:Journal of Medicinal Chemistry, 页码:5958-5963 , 文章类型: 研究论文,,卷期:2008年51-19]
- The protein kinase C (PKC) family of serine/threonine kinases is implicated in a wide variety of cellular processes. The PKC theta (PKCq) isoform is involved in TCR signal transduction and T cell activation and regulate...
- Flexible Cyclic Ethers/Polyethers as Novel P2-Ligands for HIV-1 Protease Inhibitors: Design, Synthesis, Biological Evaluation, and Protein-Ligand X-ray Studies.
[作者:Ghosh, Arun K.;Gemma, Sandra;Baldridge, Abigail;Wang, Yuan-Fang;Kovalevsky, Andrey Yu.;Koh, Yashiro;Weber, Irene T.;Mitsuya, Hiroaki;,期刊:Journal of Medicinal Chemistry, 页码:6021-6033 , 文章类型: 研究论文,,卷期:2008年51-19]
- We report the design, synthesis, and biol. evaluation of a series of novel HIV-1 protease inhibitors. The inhibitors incorporate stereochem. defined flexible cyclic ethers/polyethers as high affinity P2-ligands. Inhibit...
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