- 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...
- 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...
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