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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41条记录   Synthesis and Evaluation of Novel Boron-Containing Complexes of Potential Use for the Selective Treatment of Malignant Melanoma. [作者：Bonjoch, Josep;Drew, Michael G. B.;Gonzalez, Asensio;Greco, Francesca;Jawaid, Samaila;Osborn, Helen M. I.;Williams, Nana Aba O.;Yaqoob, Parveen;,期刊：Journal of Medicinal Chemistry, 页码：6604-6608 , 文章类型： 研究论文，,卷期：2008年51-20] Boron-contg. complexes that have the potential to irreversibly accumulate in melanoma cells have been prepd. by reaction of amino acids with 9-methoxy-9-borabicyclo[3.3.1]nonane. The ability of each complex to act as a ... 5-N-Methylated Quindoline Derivatives as Telomeric G-Quadruplex Stabilizing Ligands: Effects of 5-N Positive Charge on Quadruplex Binding Affinity and Cell Proliferation. [作者：Lu, Yu-Jing;Ou, Tian-Miao;Tan, Jia-Heng;Hou, Jin-Qiang;Shao, Wei-Yan;Peng, Dan;Sun, Ning;Wang, Xiao-Dong;Wu, Wei-Bin;Bu, Xian-Zhang;Huang, Zhi-Shu;Ma, Dik-Lung;Wong, Kwok-Yin;Gu, Lian-Quan;,期刊：Journal of Medicinal Chemistry, 页码：6381-6392 , 文章类型： 研究论文，,卷期：2008年51-20] A series of 5-N-Me quindoline (cryptolepine) derivs. as telomeric quadruplex ligands was synthesized and evaluated. The designed ligands possess a pos. charge at the 5-N position of the arom. quindoline scaffold. The q... Bornyl- and Isobornyl-D8-tetrahydrocannabinols: A Novel Class of Cannabinergic Ligands. [作者：Lu, Dai;Guo, Jianxian;Duclos, Richard I.;Bowman, Anna L.;Makriyannis, Alexandros;,期刊：Journal of Medicinal Chemistry, 页码：6393-6399 , 文章类型： 研究论文，,卷期：2008年51-20] Structure-activity relationship studies of classical cannabinoid analogs have established that the C3 aliph. side chain plays a pivotal role in detg. cannabinergic potency. In earlier work, we provided evidence for the ... Discovery of Bioavailable 4,4-Disubstituted Piperidines as Potent Ligands of the Chemokine Receptor 5 and Inhibitors of the Human Immunodeficiency Virus-1. [作者：Kazmierski, Wieslaw M.;Aquino, Christopher;Chauder, Brian A.;Deanda, Felix;Ferris, Robert;Jones-Hertzog, Deborah K.;Kenakin, Terrence;Koble, Cecilia S.;Watson, Christian;Wheelan, Pat;Yang, Hanbiao;Youngman, Michael;,期刊：Journal of Medicinal Chemistry, 页码：6538-6546 , 文章类型： 研究论文，,卷期：2008年51-20] We describe robust chem. approaches toward putative CCR5 scaffolds designed in our labs. Evaluation of analogs in the 125I-[MIP-1b] binding and Ba-L-HOS antiviral assays resulted in the discovery of 64 and 68 in the 4,4... Isosorbide-2-carbamate Esters: Potent and Selective Butyrylcholinesterase Inhibitors. [作者：Carolan, Ciaran G.;Dillon, Gerald P.;Gaynor, Joanne M.;Reidy, Sean;Ryder, Sheila A.;Khan, Denise;Marquez, Juan F.;Gilmer, John F.;,期刊：Journal of Medicinal Chemistry, 页码：6400-6409 , 文章类型： 研究论文，,卷期：2008年51-20] In this study, the authors report the SAR and characterization of two groups of isosorbide-based cholinesterase inhibitors. The first was retention of the 5-nitrate group and introduction of a series of 2-carbamate func... Rotationally Constrained 2,4-Diamino-5,6-disubstituted Pyrimidines: A New Class of Histamine H4 Receptor Antagonists with Improved Druglikeness and in Vivo Efficacy in Pain and Inflammation Models. [作者：Cowart, Marlon D.;Altenbach, Robert J.;Liu, Huaqing;Hsieh, Gin C.;Drizin, Irene;Milicic, Ivan;Miller, Thomas R.;Witte, David G.;Wishart, Neil;Fix-Stenzel, Shannon R.;McPherson, Michael J.;Adair, Ronald M.;Wetter, Jill M.;Bettencourt, Brian M.;Marsh, Kenna,期刊：Journal of Medicinal Chemistry, 页码：6547-6557 , 文章类型： 研究论文，,卷期：2008年51-20] designed based on rotationally restricted 2,4-diaminopyrimidines. Series compds. showed potent and selective in vitro H4 antagonism across multiple species, good CNS penetration, improved PK properties compared to ref. H... Discovery of Highly Selective and Potent p38 Inhibitors Based on a Phthalazine Scaffold. [作者：Herberich, Brad;Cao, Guo-Qiang;Chakrabarti, Partha P.;Falsey, James R.;Pettus, Liping;Rzasa, Robert M.;Reed, Anthony B.;Reichelt, Andreas;Sham, Kelvin;Thaman, Maya;Wurz, Ryan P.;Xu, Shimin;Zhang, Dawei;Hsieh, Faye;Lee, Matthew R.;Syed, Rashid;Li, Vivian;G,期刊：Journal of Medicinal Chemistry, 页码：6271-6279 , 文章类型： 研究论文，,卷期：2008年51-20] Investigations into the structure-activity relationships (SAR) of a series of phthalazine-based inhibitors of p38 are described. These efforts originated from quinazoline 1 and through rational design led to the develop... Discovery of Novel PPAR Ligands by a Virtual Screening Approach Based on Pharmacophore Modeling, 3D Shape, and Electrostatic Similarity Screening. [作者：Markt, Patrick;Petersen, Rasmus K.;Flindt, Esben N.;Kristiansen, Karsten;Kirchmair, Johannes;Spitzer, Gudrun;Distinto, Simona;Schuster, Daniela;Wolber, Gerhard;Laggner, Christian;Langer, Thierry;,期刊：Journal of Medicinal Chemistry, 页码：6303-6317 , 文章类型： 研究论文，,卷期：2008年51-20] Peroxisome proliferator-activated receptors (PPARs) are important targets for drugs used in the treatment of atherosclerosis, dyslipidemia, obesity, type 2 diabetes, and other diseases caused by abnormal regulation of th... Conjugated Chitosan as a Novel Platform for Oral Delivery of Paclitaxel. [作者：Lee, Eunhye;Lee, Jinju;Lee, In-Hyun;Yu, Mikyung;Kim, Hyungjun;Chae, Su Young;Jon, Sangyong;,期刊：Journal of Medicinal Chemistry, 页码：6442-6449 , 文章类型： 研究论文，,卷期：2008年51-20] A new platform for oral delivery of paclitaxel (PTX) was developed through chem. conjugation of PTX to a low mol. wt. chitosan (LMWC). The LMWC-PTX conjugate contained ~12 wt. % PTX and showed greatly enhanced water soly... Intracellular Trapping of cycloSal-Pronucleotides: Modification of Prodrugs with Amino Acid Esters. [作者：Jessen, Henning J.;Balzarini, Jan;Meier, Chris;,期刊：Journal of Medicinal Chemistry, 页码：6592-6598 , 文章类型： 研究论文，,卷期：2008年51-20] A new class of d4TMP-cycloSal-pronucleotides bearing enzymically cleavable amino acid esters is reported. These compds. are designed to trap the pronucleotide inside the cell by a fast conversion of a nonpolar ester gro... Synthesis and Utilization of Chiral a-Methylated a-Amino Acids with a Carboxyalkyl Side Chain in the Design of Novel Grb2-SH2 Peptide Inhibitors Free of Phosphotyrosine. [作者：Long, Ya-Qiu;Xue, Ting;Song, Yan-Li;Liu, Zu-Long;Huang, Shao-Xu;Yu, Qiang;,期刊：Journal of Medicinal Chemistry, 页码：6371-6380 , 文章类型： 研究论文，,卷期：2008年51-20] The growth factor receptor-bound protein 2 (Grb2) is an SH2 domain-contg. docking module that represents an attractive target for anticancer therapeutic intervention. To improve the potency and bioavailability of the Gr... Discovery of 3-{5-[(6-Amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chloropheno xy}-5-chlorobenzonitrile (MK-4965): A Potent, Orally Bioavailable HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitor with Improved Potency against Key Mutant Viruses. [作者：Tucker, Thomas J.;Sisko, John T.;Tynebor, Robert M.;Williams, Theresa M.;Felock, Peter J.;Flynn, Jessica A.;Lai, Ming-Tain;Liang, Yuexia;McGaughey, Georgia;Liu, Meiquing;Miller, Mike;Moyer, Gregory;Munshi, Vandna;Perlow-Poehnelt, Rebecca;Prasad, Sridhar;R,期刊：Journal of Medicinal Chemistry, 页码：6503-6511 , 文章类型： 研究论文，,卷期：2008年51-20] Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have been shown to be a key component of highly active antiretroviral therapy (HAART). The use of NNRTIs has become part of std. combination antiviral therapies p... Design, Synthesis, and Biological Evaluation of Novel Constrained meta-Substituted Phenyl Propanoic Acids as Peroxisome Proliferator-Activated Receptor a and g Dual Agonists. [作者：Suh, Young-Ger;Kim, Nam-Jung;Koo, Bon-Woong;Lee, Kwang-Ok;Moon, Sung-Hyun;Shin, Dong-Hyung;Jung, Jong-Wha;Paek, Seung-Mann;Chang, Dong-Jo;Li, Funan;Kang, Hyun-Jin;Le, Tuong Vy Thi;Chae, Yu Na;Shin, Chang Yell;Kim, Mi-Kyung;Lim, Joong In;Ryu, Jae-Sang;Park,期刊：Journal of Medicinal Chemistry, 页码：6318-6333 , 文章类型： 研究论文，,卷期：2008年51-20] In an effort to develop dual PPARa/g activators with improved therapeutic efficacy, a series of diaryl a-ethoxy propanoic acid compds. comprising two aryl groups linked by rigid oxime ether or isoxazoline ring were desig... Identification of a Nonbasic, Nitrile-Containing Cathepsin K Inhibitor (MK-1256) that is Efficacious in a Monkey Model of Osteoporosis. [作者：Robichaud, Joel;Black, W. Cameron;Therien, Michel;Paquet, Julie;Oballa, Renata M.;Bayly, Christopher I.;McKay, Daniel J.;Wang, Qingping;Isabel, Elise;Leger, Serge;Mellon, Christophe;Kimmel, Donald B.;Wesolowski, Gregg;Percival, M. David;Masse, Frederic;De,期刊：Journal of Medicinal Chemistry, 页码：6410-6420 , 文章类型： 研究论文，,卷期：2008年51-20] Herein, the authors report on the identification of nonbasic, potent, and highly selective, nitrile-contg. cathepsin K (Cat K) inhibitors that are built on the previously identified cyclohexanecarboxamide core structure.... Ni(II), Cu(II), and Zn(II) Diethyldithiocarbamate Complexes Show Various Activities Against the Proteasome in Breast Cancer Cells. [作者：Cvek, Boris;Milacic, Vesna;Taraba, Jan;Dou, Q. Ping;,期刊：Journal of Medicinal Chemistry, 页码：6256-6258 , 文章类型： 研究论文，,卷期：2008年51-20] Three complexes with diethyldithiocarbamate ligand and three different metals (Ni, Cu, Zn) were prepd., confirmed by x-ray crystallog., and tested in human breast cancer MDA-MB-231 cells. Zn and Cu complexes, but not Ni... Gedunin, a Novel Hsp90 Inhibitor: Semisynthesis of Derivatives and Preliminary Structure-Activity Relationships. [作者：Brandt, Gary E. L.;Schmidt, Matthew D.;Prisinzano, Thomas E.;Blagg, Brian S. J.;,期刊：Journal of Medicinal Chemistry, 页码：6495-6502 , 文章类型： 研究论文，,卷期：2008年51-20] Gedunin, a tetranortriterpenoid isolated from the Indian neem tree (Azadirachta indica), was recently shown to manifest anticancer activity via inhibition of the 90 kDa heat shock protein (Hsp90) folding machinery and to...