Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1) (English)
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In:
Bioorganic and Medicinal Chemistry Letters
;
21
, 22
;
6693-6698
;
2011
-
ISSN:
- Article (Journal) / Electronic Resource
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Title:Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1)
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Contributors:Wu, Shung C. ( author ) / Yoon, David ( author ) / Chin, Janice ( author ) / van Kirk, Katy ( author ) / Seethala, Ramakrishna ( author ) / Golla, Rajasree ( author ) / He, Bin ( author ) / Harrity, Thomas ( author ) / Kunselman, Lori K. ( author ) / Morgan, Nathan N. ( author )
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Published in:Bioorganic and Medicinal Chemistry Letters ; 21, 22 ; 6693-6698
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Publisher:
- New search for: Elsevier Ltd
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Publication date:2011-09-15
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Size:6 pages
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ISSN:
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DOI:
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Type of media:Article (Journal)
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Type of material:Electronic Resource
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Language:English
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Keywords:
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Source:
Table of contents – Volume 21, Issue 22
The tables of contents are generated automatically and are based on the data records of the individual contributions available in the index of the TIB portal. The display of the Tables of Contents may therefore be incomplete.
- 6615
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Graphical contents list| 2011
- 6630
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Molecular dynamics simulations and MM/GBSA methods to investigate binding mechanisms of aminomethylpyrimidine inhibitors with DPP-IVDesheng, Liang / Jian, Gao / Yuanhua, Cheng / Wei, Cui / Huai, Zhang / Mingjuan, Ji et al. | 2011
- 6636
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A double prodrug system for colon targeting of benzenesulfonamide COX-2 inhibitorsMarquez Ruiz, Juan F. / Kedziora, Kinga / Keogh, Brian / Maguire, Jacqueline / Reilly, Mary / Windle, Henry / Kelleher, Dermot P. / Gilmer, John F. et al. | 2011
- 6641
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A modular approach to trim cellular targets in anticancer drug discoveryRíos-Luci, Carla / Domínguez-Kelly, Raquel / León, Leticia G. / Díaz-Rodríguez, Elena / Freire, Raimundo / Pandiella, Atanasio / Cikotiene, Inga / Padrón, José M. et al. | 2011
- 6646
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7-Oxopyrrolopyridine-derived DPP4 inhibitors—mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active siteWang, Wei / Devasthale, Pratik / Wang, Aiying / Harrity, Tom / Egan, Don / Morgan, Nathan / Cap, Michael / Fura, Aberra / Klei, Herbert E. / Kish, Kevin et al. | 2011
- 6652
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Synthesis and structure–activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitorsGewald, Rainer / Rueger, Carla / Grunwald, Christian / Egerland, Ute / Hoefgen, Norbert et al. | 2011
- 6657
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Carbazole-containing arylcarboxamides as BACE1 inhibitorsBertini, Simone / Asso, Valentina / Ghilardi, Elisa / Granchi, Carlotta / Manera, Clementina / Minutolo, Filippo / Saccomanni, Giuseppe / Bortolato, Andrea / Mason, Jonathan / Moro, Stefano et al. | 2011
- 6662
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Synthesis and anti-tumor activities of Nprime-benzylidene-2-(4-oxothieno[2,3-d]pyrimidin-3(4H)-yl)acetohydrazone derivativesLou, J. / Liu, Z. / Li, Y. / Zhou, M. / Zhang, Z. / Zheng, S. / Wang, R. / Li, J. et al. | 2011
- 6662
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Synthesis and anti-tumor activities of N′-benzylidene-2-(4-oxothieno[2,3-d]pyrimidin-3(4H)-yl)acetohydrazone derivativesLou, Jiangping / Liu, Zhen / Li, Yan / Zhou, Mi / Zhang, Zhengxi / Zheng, Shu / Wang, Renxiao / Li, Jian et al. | 2011
- 6667
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Functional characterization of rat glutaryl-CoA dehydrogenase and its comparison with straight-chain acyl-CoA dehydrogenaseWu, Long / Qiao, Yuqin / Gao, Jinbo / Deng, Guisheng / Yu, Wenhua / Chen, Gong / Li, Ding et al. | 2011
- 6674
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Synthesis and acrosin inhibitory activity of substituted 4-amino-N-(diaminomethylene) benzenesulfonamide derivativesDing, Lili / Zhu, Ju / Zheng, Canhui / Sheng, Chunquan / Qi, Jingjing / Liu, Xuefei / Han, Guangqian / Zhao, Juntao / Lv, Jiaguo / Zhou, Youjun et al. | 2011
- 6678
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Synthesis of polyfunctionalized piperidone oxime ethers and their cytotoxicity on HeLa cellsParthiban, Paramasivam / Pallela, Ramjee / Kim, Se-Kwon / Park, Dong Ho / Jeong, Yeon Tae et al. | 2011
- 6687
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7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: A novel class of Pim kinase inhibitors with potent cell antiproliferative activityPierre, Fabrice / Stefan, Eric / Nédellec, Anne-Sophie / Chevrel, Marie-Claire / Regan, Collin F. / Siddiqui-Jain, Adam / Macalino, Diwata / Streiner, Nicole / Drygin, Denis / Haddach, Mustapha et al. | 2011
- 6693
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Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11b-hydroxydehydrogenase 1 (11b-HSD1)Wu, S. C. / Yoon, D. / Chin, J. / van Kirk, K. / Seethala, R. / Golla, R. / He, B. / Harrity, T. / Kunselman, L. K. / Morgan, N. N. et al. | 2011
- 6693
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Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1)Wu, Shung C. / Yoon, David / Chin, Janice / van Kirk, Katy / Seethala, Ramakrishna / Golla, Rajasree / He, Bin / Harrity, Thomas / Kunselman, Lori K. / Morgan, Nathan N. et al. | 2011
- 6699
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Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11b-hydroxysteroid dehydrogenase type 1 (11b-HSD-1)Ye, X. Y. / Chen, S. Y. / Nayeem, A. / Golla, R. / Seethala, R. / Wang, M. / Harper, T. / Sleczka, B. G. / Li, Y. X. / He, B. et al. | 2011
- 6699
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Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1)Ye, Xiang-Yang / Chen, Stephanie Y. / Nayeem, Akbar / Golla, Rajasree / Seethala, Ramakrishna / Wang, Mengmeng / Harper, Timothy / Sleczka, Bogdan G. / Li, Yi-Xin / He, Bin et al. | 2011
- 6705
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Identification of a novel RAMP-independent CGRP receptor antagonistZartman, C. Blair / Bell, Ian M. / Gallicchio, Steven N. / Graham, Samuel L. / Kane, Stefanie A. / Mallee, John J. / Rutledge, Ruth Z. / Salvatore, Christopher A. / Vacca, Joseph P. / Williams, Theresa M. et al. | 2011
- 6709
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Discovery and synthesis of novel substituted benzocoumarins as orally active lipid modulating agentsSashidhara, Koneni V. / Kumar, Manoj / Modukuri, Ram K. / Srivastava, Anuj / Puri, Anju et al. | 2011
- 6714
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A novel potential therapeutic avenue for autism: Design, synthesis and pharmacophore generation of SSRIs with dual actionGhoneim, Ola M. / Ibrahim, Diaa A. / El-Deeb, Ibrahim M. / Lee, So Ha / Booth, Raymond G. et al. | 2011
- 6724
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Rational design of 2-pyrrolinones as inhibitors of HIV-1 integraseMa, Kaiqing / Wang, Penghui / Fu, Wei / Wan, Xiaolong / Zhou, Lu / Chu, Yong / Ye, Deyong et al. | 2011
- 6728
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One-class classification as a novel method of ligand-based virtual screening: The case of glycogen synthase kinase 3β inhibitorsKarpov, Pavel V. / Osolodkin, Dmitry I. / Baskin, Igor I. / Palyulin, Vladimir A. / Zefirov, Nikolay S. et al. | 2011
- 6728
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One-class classification as a novel method of ligand-based virtual screening: The case of glycogen synthase kinase 3b inhibitorsKarpov, P. V. / Osolodkin, D. I. / Baskin, I. I. / Palyulin, V. A. / Zefirov, N. S. et al. | 2011
- 6732
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Synthesis and antibacterial activity of N 4-mono alkyl derivatives of novel glycopeptide LYV07ww01Shao, Chang / Zhou, Weicheng / Zhang, Shunli / Wei, Wei / Ruan, Lingao / Jin, Yiping / Sun, Xinqiang / Huang, Yanqin et al. | 2011
- 6739
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Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotypeUrbano, Mariangela / Guerrero, Miguel / Velaparthi, Subash / Crisp, Melissa / Chase, Peter / Hodder, Peter / Schaeffer, Marie-Therese / Brown, Steven / Rosen, Hugh / Roberts, Edward et al. | 2011
- 6746
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Effect of the leukotriene A4 hydrolase aminopeptidase augmentor 4-methoxydiphenylmethane in a pre-clinical model of pulmonary emphysemaDe Oliveira, Eliseu O. / Wang, Kan / Kong, Hye-Sik / Kim, Suhyon / Miessau, Matthew / Snelgrove, Robert J. / Shim, Y. Michael / Paige, Mikell et al. | 2011
- 6751
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Designing 2-aminoimidazole alkaloids analogs with anti-biofilm activities: Structure–activities relationships of polysubstituted triazolesLinares, D. / Bottzeck, O. / Pereira, O. / Praud-Tabariès, A. / Blache, Y. et al. | 2011
- 6756
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Synthesis and radioligand binding studies of bis-(8-isopropyl-isoquinolinium) derivatives as ligands for apamin-sensitive sites on cloned SK2 and SK3 channelsBadarau, Eduard / Dilly, Sébastien / Dufour, Fabien / Poncin, Sylvie / Seutin, Vincent / Liégeois, Jean-François et al. | 2011
- 6760
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Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA)Matthews, Hayden / Ranson, Marie / Tyndall, Joel D.A. / Kelso, Michael J. et al. | 2011
- 6767
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4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitorsRossi, Cristina / Fincham, Christopher I. / D’Andrea, Piero / Porcelloni, Marina / Ettorre, Alessandro / Mauro, Sandro / Bigioni, Mario / Binaschi, Monica / Maggi, Carlo A. / Nardelli, Federica et al. | 2011
- 6770
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Synthesis and anti-HIV-1 activity of 4-substituted-7-(2′-deoxy-2′-fluoro-4′-azido-β-d-ribofuranosyl)pyrrolo[2,3-d]pyrimidine analoguesGuo, Xiaohe / Li, Yujiang / Tao, Le / Wang, Qiang / Wang, Shuyang / Hu, Weidong / Pan, Zhenliang / Yang, Qinghua / Cui, Yanmei / Ge, Zhaopeng et al. | 2011
- 6770
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Synthesis and anti-HIV-1 activity of 4-substituted-7-(2prime-deoxy-2prime-fluoro-4prime-azido-b-d-ribofuranosyl)pyrrolo[2,3-d]pyrimidine analoguesGuo, X. / Li, Y. / Tao, L. / Wang, Q. / Wang, S. / Hu, W. / Pan, Z. / Yang, Q. / Cui, Y. / Ge, Z. et al. | 2011
- 6773
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Discovery of a new class of glucosylceramide synthase inhibitorsKoltun, Elena / Richards, Steven / Chan, Vicky / Nachtigall, Jason / Du, Hongwang / Noson, Kevin / Galan, Adam / Aay, Naing / Hanel, Art / Harrison, Amanda et al. | 2011
- 6778
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Acid mediated formation of an N-acyliminium ion from tubulysins: A new methodology for the synthesis of natural tubulysins and their analogsVlahov, Iontcho R. / Wang, Yu / Vetzel, Marilynn / Hahn, Spencer / Kleindl, Paul J. / Reddy, Joseph A. / Leamon, Christopher P. et al. | 2011
- 6782
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The design, synthesis and biological evaluation of novel URB602 analogues as potential monoacylglycerol lipase inhibitorsSzabo, Monika / Agostino, Mark / Malone, Daniel T. / Yuriev, Elizabeth / Capuano, Ben et al. | 2011
- 6788
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Synthesis of purine modified 2′-C-methyl nucleosides as potential anti-HCV agentsZhang, Hong-wang / Zhou, Longhu / Coats, Steven J. / McBrayer, Tamara R. / Tharnish, Phillip M. / Bondada, Lavanya / Detorio, Mervi / Amichai, Sarah A. / Johns, Melissa D. / Whitaker, Tony et al. | 2011
- 6788
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Synthesis of purine modified 2prime-C-methyl nucleosides as potential anti-HCV agentsZhang, H. w. / Zhou, L. / Coats, S. J. / McBrayer, T. R. / Tharnish, P. M. / Bondada, L. / Detorio, M. / Amichai, S. A. / Johns, M. D. / Whitaker, T. et al. | 2011
- 6793
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Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitorsMortensen, Deborah S. / Perrin-Ninkovic, Sophie M. / Harris, Roy / Lee, Branden G.S. / Shevlin, Graziella / Hickman, Matt / Khambatta, Gody / Bisonette, Rene R. / Fultz, Kimberly E. / Sankar, Sabita et al. | 2011
- 6800
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Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibitionHu, Yonghan / Xing, Li / Thomason, Jennifer R. / Xiang, Jason / Ipek, Manus / Guler, Satenig / Li, Huanqiu / Sabatini, Joshua / Chockalingam, Priya / Reifenberg, Erica et al. | 2011
- 6804
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Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivativesLi, Yang-Biao / Xie, Yun-Ying / Du, Na-Na / Lu, Yu / Xu, Hong-Zhang / Wang, Bin / Yu, Ying / Liu, Yan-Xin / Song, Dan-Qing / Chen, Ru-Xian et al. | 2011
- 6808
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New bioactive macrocyclic diterpenoids from Jatropha multifidaKanth, Boddu Shashi / Kumar, Avula Satya / Shinde, Digambar Balaji / Babu, Kothapalli Hari / Raju, Tuniki Venugopal / Kumar, Chityal Ganesh / Sujitha, Pombala / Das, Biswanath et al. | 2011
- 6811
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Synthesis and antioxidant activities of novel 4-Schiff base-7-benzyloxy-coumarin derivativesZhang, Ye / Zou, Biqun / Chen, Zhenfeng / Pan, Yingming / Wang, Hengshan / Liang, Hong / Yi, Xianghui et al. | 2011
- 6816
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Protein binding site analysis by means of structural interaction fingerprint patternsMordalski, Stefan / Kosciolek, Tomasz / Kristiansen, Kurt / Sylte, Ingebrigt / Bojarski, Andrzej J. et al. | 2011
- 6820
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Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-N′-[4-(2-fluoroethoxy)benzyl]piperazine, a novel σ 1 receptor PET imaging agentMoussa, Iman A. / Banister, Samuel D. / Giboureau, Nicolas / Meikle, Steven R. / Kassiou, Michael et al. | 2011
- 6820
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Synthesis and in vivo evaluation of [18F]N-(2-benzofuranylmethyl)-Nprime-[4-(2-fluoroethoxy)benzyl]piperazine, a novel 1 receptor PET imaging agentMoussa, I. A. / Banister, S. D. / Giboureau, N. / Meikle, S. R. / Kassiou, M. et al. | 2011
- 6824
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Structural requirement of phenylthiourea analogs for their inhibitory activity of melanogenesis and tyrosinaseThanigaimalai, Pillaiyar / Lee, Ki-Cheul / Sharma, Vinay K. / Joo, Cheonik / Cho, Won-Jea / Roh, Eunmiri / Kim, Youngsoo / Jung, Sang-Hun et al. | 2011
- 6829
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Structure–activity relationship study of arylsulfonylimidazolidinones as anticancer agentsSharma, Vinay K. / Lee, Ki-Cheul / Venkateswararao, Eeda / Joo, Cheonik / Kim, Min-Seok / Sharma, Niti / Jung, Sang-Hun et al. | 2011
- 6833
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Fatty acids as natural specific inhibitors of the proto-oncogenic protein Shp2Liu, Dongping / Kong, Guiping / Chen, Quan Cheng / Wang, Guanghui / Li, Jie / Xu, Yang / lin, Ting / Tian, Yingpu / Zhang, Xiaokun / Yao, Xinsheng et al. | 2011
- 6838
-
Investigating the role of the hydroxyl groups of substrate erythrose 4-phosphate in the reaction catalysed by the first enzyme of the shikimate pathwayTran, David / Pietersma, Amy L. / Schofield, Linley R. / Rost, Matthias / Jameson, Geoffrey B. / Parker, Emily J. et al. | 2011
- 6842
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Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophoresBetageri, Raj / Gilmore, Thomas / Kuzmich, Daniel / Kirrane, Thomas M. / Bentzien, Jörg / Wiedenmayer, Dieter / Bekkali, Younes / Regan, John / Berry, Angela / Latli, Bachir et al. | 2011
- 6852
-
Discovery of highly potent small molecule Hepatitis C Virus entry inhibitorsMittapalli, Gopi Kumar / Jackson, Andrew / Zhao, Fang / Lee, Haekyung / Chow, Stephine / McKelvy, Jeffrey / Wong-Staal, Flossie / Macdonald, James E. et al. | 2011
- 6856
-
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studiesYang, Yifan / Miller, Keith J. / Zhu, Yeheng / Hong, Yang / Tian, Yuan / Murugesan, Natesan / Gu, Zhengxiang / O’Tanyi, Eva / Keim, William J. / Rohrbach, Kenneth W. et al. | 2011
- 6861
-
Identification of 4-quinolone derivatives as inhibitors of reactive oxygen species production from human umbilical vein endothelial cellsOnda, Kenichi / Narazaki, Fumie / Ishibashi, Naoki / Nakanishi, Keita / Sawada, Yuki / Imamura, Ken-ichiro / Momose, Kazuhiro / Furukawa, Shigetada / Shimada, Yoshiaki / Moriguchi, Hiroyuki et al. | 2011
- 6867
-
Computational techniques are valuable tools for the discovery of protein–protein interaction inhibitors: The 14-3-3σ caseCorradi, Valentina / Mancini, Manuela / Santucci, Maria Alessandra / Carlomagno, Teresa / Sanfelice, Domenico / Mori, Mattia / Vignaroli, Giulia / Falchi, Federico / Manetti, Fabrizio / Radi, Marco et al. | 2011
- 6872
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A fluorescent probe for GM1 gangliosidosis related b-galactosidase: N-(Dansylamino)hexylaminocarbonylpentyl-1,5-dideoxy-1,5-imino-d-galactitolFrohlich, R. F. / Fantur, K. / Furneaux, R. H. / Paschke, E. / Stutz, A. E. / Wicki, J. / Withers, S. G. / Wrodnigg, T. M. et al. | 2011
- 6872
-
A fluorescent probe for GM1 gangliosidosis related β-galactosidase: N-(Dansylamino)hexylaminocarbonylpentyl-1,5-dideoxy-1,5-imino-d-galactitolFröhlich, Richard F.G. / Fantur, Katrin / Furneaux, Richard H. / Paschke, Eduard / Stütz, Arnold E. / Wicki, Jacqueline / Withers, Stephen G. / Wrodnigg, Tanja M. et al. | 2011
- 6876
-
AHL-dependent quorum sensing inhibition: Synthesis and biological evaluation of α-(N-alkyl-carboxamide)-γ-butyrolactones and α-(N-alkyl-sulfonamide)-γ-butyrolactonesBoukraa, Mohamed / Sabbah, Mohamad / Soulère, Laurent / El Efrit, Mohamed L. / Queneau, Yves / Doutheau, Alain et al. | 2011
- 6876
-
AHL-dependent quorum sensing inhibition: Synthesis and biological evaluation of a-(N-alkyl-carboxamide)-g-butyrolactones and a-(N-alkyl-sulfonamide)-g-butyrolactonesBoukraa, M. / Sabbah, M. / Soulere, L. / El Efrit, M. L. / Queneau, Y. / Doutheau, A. et al. | 2011
- 6880
-
Pt-rotaxanes as cytotoxic agentsWang, Xiaoyang / Smithrud, David B. et al. | 2011
- 6884
-
Inhibitory effect on NO production of phenolic compounds from Myristica fragransCuong, To Dao / Hung, Tran Manh / Na, MinKyun / Ha, Do Thi / Kim, Jin Cheol / Lee, Dongho / Ryoo, SungWoo / Lee, Jeong Hyung / Choi, Jae Sue / Min, Byung Sun et al. | 2011
- 6888
-
Identification and SAR of selective inducible nitric oxide synthase (iNOS) dimerization inhibitorsGahman, Timothy C. / Herbert, Mark R. / Lang, Henk / Thayer, Angie / Symons, Kent T. / Nguyen, Phan Manh / Massari, Mark E. / Dozier, Sara / Zhang, Yan / Sablad, Marciano et al. | 2011
- 6895
-
Design, synthesis, and biological activity of a novel series of 2,5-disubstituted furans/pyrroles as HIV-1 fusion inhibitors targeting gp41Jiang, Shibo / Tala, Srinivasa R. / Lu, Hong / Zou, Peng / Avan, Ilker / Ibrahim, Tarek S. / Abo-Dya, Nader E. / Abdelmajeid, Abdelmotaal / Debnath, Asim K. / Katritzky, Alan R. et al. | 2011
- 6899
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Identification of novel NK1/NK3 dual antagonists for the potential treatment of schizophreniaCatalani, Maria Pia / Alvaro, Giuseppe / Bernasconi, Giovanni / Bettini, Ezio / Bromidge, Steven M. / Heer, Jag / Tedesco, Giovanna / Tommasi, Simona et al. | 2011
- 6905
-
The detection of a transgenic soybean biochip using gold label silver stain technologyDeng, Zhongliang / Ge, Yuetao / Cao, Qike / Han, Ke et al. | 2011
- 6909
-
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitorsThompson, Lorin A. / Shi, Jianliang / Decicco, Carl P. / Tebben, Andrew J. / Olson, Richard E. / Boy, Kenneth M. / Guernon, Jason M. / Good, Andrew C. / Liauw, Ann / Zheng, Changsheng et al. | 2011
- 6916
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Monosubstituted g-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of b-secretase (BACE)Boy, K. M. / Guernon, J. M. / Shi, J. / Toyn, J. H. / Meredith, J. E. / Barten, D. M. / Burton, C. R. / Albright, C. F. / Marcinkeviciene, J. / Good, A. C. et al. | 2011
- 6916
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Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)Boy, Kenneth M. / Guernon, Jason M. / Shi, Jianliang / Toyn, Jeremy H. / Meredith, Jere E. / Barten, Donna M. / Burton, Catherine R. / Albright, Charles F. / Marcinkeviciene, Jovita / Good, Andrew C. et al. | 2011
- IFC
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Editorial board| 2011