3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead (English)
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In:
Bioorganic & medicinal chemistry letters
;
21
, 11
; 3452-3457
;
2011
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ISSN:
- Article (Journal) / Print
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Title:3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead
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Contributors:Soth, Michael ( author ) / Abbot, Sarah / Abubakari, Allassan / Arora, Nidhi / Arzeno, Humberto / Billedeau, Roland / Dewdney, Nolan / Durkin, Kieran / Frauchiger, Sandra / Ghate, Manjiri
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Published in:Bioorganic & medicinal chemistry letters ; 21, 11 ; 3452-3457
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Publisher:
- New search for: Elsevier
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Place of publication:Amsterdam [u.a.]
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Publication date:2011
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ISSN:
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ZDBID:
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Type of media:Article (Journal)
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Type of material:Print
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Language:English
- New search for: 35.70 / 44.33 / 44.42
- Further information on Basic classification
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Keywords:
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Classification:
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Source:
Table of contents – Volume 21, Issue 11
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.
- 3181
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Graphical contents list| 2011
- 3198
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Actin depolymerizing effect of trisoxazole-containing macrolidesChung, Soon-Chun / Lee, So-Hyoung / Jang, Kyoung Hwa / Park, Wanki / Jeon, Ju-eun / Oh, Hana / Shin, Jongheon / Oh, Ki-Bong et al. | 2011
- 3202
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2-Arylmethylaminomethyl-5,6-dihydroxychromone derivatives with selective anti-HCV activityPark, Hye Ri / Park, Kwang-Su / Chong, Youhoon et al. | 2011
- 3206
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Design and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide cleavage processHakamata, Wataru / Machida, Aki / Oku, Tadatake / Nishio, Toshiyuki et al. | 2011
- 3210
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4-Aminothiazolyl analogs of GE2270 A: Design, synthesis and evaluation of imidazole analogsLaMarche, Matthew J. / Leeds, Jennifer A. / Dzink-Fox, JoAnne / Mullin, Steve / Patane, Michael A. / Rann, Elin M. / Tiamfook, Stacey et al. | 2011
- 3216
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Synthesis and crystallographic analysis of new sulfonamides incorporating NO-donating moieties with potent antiglaucoma actionMincione, Francesco / Benedini, Francesca / Biondi, Stefano / Cecchi, Alessandro / Temperini, Claudia / Formicola, Giuseppe / Pacileo, Ilaria / Scozzafava, Andrea / Masini, Emanuela / Supuran, Claudiu T. et al. | 2011
- 3222
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Radiosynthesis of [11C]Vandetanib and [11C]chloro-Vandetanib as new potential PET agents for imaging of VEGFR in cancerGao, Mingzhang / Lola, Christian M. / Wang, Min / Miller, Kathy D. / Sledge, George W. / Zheng, Qi-Huang et al. | 2011
- 3227
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The discovery and structure–activity relationships of pyrano[3,4-b]indole-based inhibitors of hepatitis C virus NS5B polymeraseJackson, Randy W. / LaPorte, Matthew G. / Herbertz, Torsten / Draper, Tandy L. / Gaboury, Janet A. / Rippin, Susan R. / Patel, Ravi / Chunduru, Srinivas K. / Benetatos, Christopher A. / Young, Dorothy C. et al. | 2011
- 3232
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Toward self-adjuvanting subunit vaccines: Model peptide and protein antigens incorporating covalently bound toll-like receptor-7 agonistic imidazoquinolinesShukla, Nikunj M. / Lewis, Tyler C. / Day, Timothy P. / Mutz, Cole A. / Ukani, Rehman / Hamilton, Chase D. / Balakrishna, Rajalakshmi / David, Sunil A. et al. | 2011
- 3237
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Orally active aminopyridines as inhibitors of tetrameric fructose-1,6-bisphosphataseHebeisen, Paul / Haap, Wolfgang / Kuhn, Bernd / Mohr, Peter / Wessel, Hans Peter / Zutter, Ulrich / Kirchner, Stephan / Ruf, Armin / Benz, Jörg / Joseph, Catherine et al. | 2011
- 3243
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Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl seriesAlagille, David / DaCosta, Herve / Chen, Yelin / Hemstapat, Kamondanai / Rodriguez, Alice / Baldwin, Ronald M. / Conn, Jeffrey P. / Tamagnan, Gilles D. et al. | 2011
- 3248
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Osteogenic activity of diphenyl ether-type cyclic diarylheptanoids derived from Acer nikoenseYonezawa, Takayuki / Lee, Ji-Won / Akazawa, Hiroyuki / Inagaki, Masahiko / Cha, Byung-Yoon / Nagai, Kazuo / Yagasaki, Kazumi / Akihisa, Toshihiro / Woo, Je-Tae et al. | 2011
- 3252
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Monoterpenoids from the aerial parts of Aruncus dioicus var. kamtschaticus and their antioxidant and cytotoxic activitiesJeong, Su Yang / Jun, Do Youn / Kim, Young Ho / Min, Byung-Sun / Min, Bo Kyung / Woo, Mi Hee et al. | 2011
- 3257
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Synthesis of cholestane saponins as mimics of OSW-1 and their cytotoxic activitiesZheng, Dan / Guan, Yuyao / Chen, Xiaozhuo / Xu, Yanpeng / Chen, Xiaoguang / Lei, Pingsheng et al. | 2011
- 3261
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Phenolic compounds with NF-kB inhibitory effects from the fungus Phellinus baumiiWu, C. S. / Lin, Z. M. / Wang, L. N. / Guo, D. X. / Wang, S. Q. / Liu, Y. Q. / Yuan, H. Q. / Lou, H. X. et al. | 2011
- 3261
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Phenolic compounds with NF-κB inhibitory effects from the fungus Phellinus baumiiWu, Chang-Sheng / Lin, Zhao-Min / Wang, Li-Ning / Guo, Dong-Xiao / Wang, Shu-Qi / Liu, Yong-Qing / Yuan, Hui-Qing / Lou, Hong-Xiang et al. | 2011
- 3268
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Research on PEGylation of porcine prothrombin for improving biostability and reducing animal immunogenicityZhou, Jian-Gang / Chen, Ying-Ming et al. | 2011
- 3273
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Structure–activity relationship of cyclic thiacarbocyanine tau aggregation inhibitorsSchafer, Kelsey N. / Murale, Dhiraj P. / Kim, Kibong / Cisek, Katryna / Kuret, Jeff / Churchill, David G. et al. | 2011
- 3277
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Norcantharidin analogues with nematocidal activity in Haemonchus contortusCampbell, Bronwyn E. / Tarleton, Mark / Gordon, Christopher P. / Sakoff, Jennette A. / Gilbert, Jayne / McCluskey, Adam / Gasser, Robin B. et al. | 2011
- 3282
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The identification of new metallo-β-lactamase inhibitor leads from fragment-based screeningVella, Peter / Hussein, Waleed M. / Leung, Eleanor W.W. / Clayton, Daniel / Ollis, David L. / Mitić, Nataša / Schenk, Gerhard / McGeary, Ross P. et al. | 2011
- 3282
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The identification of new metallo-b-lactamase inhibitor leads from fragment-based screeningVella, P. / Hussein, W. M. / Leung, E. W. / Clayton, D. / Ollis, D. L. / Mitic, N. / Schenk, G. / McGeary, R. P. et al. | 2011
- 3286
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Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitorsRamurthy, Savithri / Aikawa, Mina / Amiri, Payman / Costales, Abran / Hashash, Ahmad / Jansen, Johanna M. / Lin, Song / Ma, Sylvia / Renhowe, Paul A. / Shafer, Cynthia M. et al. | 2011
- 3290
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Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetesXia, Yan / Chackalamannil, Samuel / Greenlee, William J. / Jayne, Charles / Neustadt, Bernard / Stamford, Andrew / Vaccaro, Henry / Xu, Xiaoying (Lucy) / Baker, Hana / O’Neill, Kim et al. | 2011
- 3297
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Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X7 antagonistsPerez-Medrano, Arturo / Donnelly-Roberts, Diana L. / Florjancic, Alan S. / Nelson, Derek W. / Li, Tongmei / Namovic, Marian T. / Peddi, Sridhar / Faltynek, Connie R. / Jarvis, Michael F. / Carroll, William A. et al. | 2011
- 3301
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Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritisDe Savi, Chris / Pape, Andrew / Sawyer, Yvonne / Milne, David / Davies, Chris / Cumming, John G. / Ting, Attilla / Lamont, Scott / Smith, Peter D. / Tart, Jonathon et al. | 2011
- 3307
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Phosphodiesterase inhibitors. Part 1: Synthesis and structure–activity relationships of pyrazolopyridine–pyridazinone PDE inhibitors developed from ibudilastAllcock, Robert W. / Blakli, Haakon / Jiang, Zhong / Johnston, Karen A. / Morgan, Keith M. / Rosair, Georgina M. / Iwase, Kazuhiko / Kohno, Yasushi / Adams, David R. et al. | 2011
- 3313
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Synthesis of 5-thiodidehydropyranylcytosine derivatives as potential anti-HIV agentsYoshimura, Yuichi / Yamazaki, Yoshiko / Saito, Yukako / Natori, Yoshihiro / Imamichi, Tomozumi / Takahata, Hiroki et al. | 2011
- 3317
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Asymmetric synthesis and biological evaluations of (+)- and (−)-6-dimethoxymethyl-1,4-dihydropyridine-3-carboxylic acid derivatives blocking N-type calcium channelsYamamoto, Takashi / Ohno, Seiji / Niwa, Seiji / Tokumasu, Munetaka / Hagihara, Masako / Koganei, Hajime / Fujita, Shin-ichi / Takeda, Tomoko / Saitou, Yuki / Iwayama, Satoshi et al. | 2011
- 3320
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Production of doramectin by rational engineering of the avermectin biosynthetic pathwayWang, Jian-Bo / Pan, Hai-Xue / Tang, Gong-Li et al. | 2011
- 3324
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N-Hydroxy-Nprime-aminoguanidines as anti-cancer lead molecule: QSAR, synthesis and biological evaluationBasu, A. / Sinha, B. N. / Saiko, P. / Graser, G. / Szekeres, T. et al. | 2011
- 3324
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N-Hydroxy-N′-aminoguanidines as anti-cancer lead molecule: QSAR, synthesis and biological evaluationBasu, Arijit / Sinha, Barij N. / Saiko, Philipp / Graser, Geraldine / Szekeres, Thomas et al. | 2011
- 3329
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Discovery of novel HCV polymerase inhibitors using pharmacophore-based virtual screeningKim, Nam Doo / Chun, Haarin / Park, Sang Jin / Yang, Jae Won / Kim, Jong Woo / Ahn, Soon Kil et al. | 2011
- 3335
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Identification of plasmepsin inhibitors as selective anti-malarial agents using ligand based drug designMcKay, Paul B / Peters, Martin B. / Carta, Giorgio / Flood, Christopher T. / Dempsey, Enda / Bell, Angus / Berry, Colin / Lloyd, David G. / Fayne, Darren et al. | 2011
- 3342
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New halogenated phenylcoumarins as tyrosinase inhibitorsMatos, Maria João / Santana, Lourdes / Uriarte, Eugenio / Delogu, Giovanna / Corda, Marcella / Fadda, Maria Benedetta / Era, Benedetta / Fais, Antonella et al. | 2011
- 3346
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Synthesis and characterisation of a novel tubulin-directed DO3A–colchicine conjugate with potential theranostic featuresWardle, Nicholas. J. / Kalber, Tammy / Bell, Jimmy D. / Bligh, S.W. Annie et al. | 2011
- 3349
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NMR evaluation of interactions between substituted-indole and PDZ1 domain of PSD-95Vogrig, Alexandre / Boucherle, Benjamin / Deokar, Hemantkumar / Thomas, Isabelle / Ripoche, Isabelle / Lian, Lu-Yun / Ducki, Sylvie et al. | 2011
- 3354
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Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinenceUrbahns, Klaus / Yura, Takeshi / Mogi, Muneto / Tajimi, Masaomi / Fujishima, Hiroshi / Masuda, Tsutomu / Yoshida, Nagahiro / Moriwaki, Toshiya / Lowinger, Timothy B. / Meier, Heinrich et al. | 2011
- 3358
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Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activityKoller, Manuel / Lingenhoehl, Kurt / Schmutz, Markus / Vranesic, Ivan-Toma / Kallen, Joerg / Auberson, Yves P. / Carcache, David A. / Mattes, Henri / Ofner, Silvio / Orain, David et al. | 2011
- 3362
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Synthesis of biotinylated muramyl tripeptides with NOD2-stimulating activityGisch, Nicolas / Buske, Birte / Heine, Holger / Lindner, Buko / Zähringer, Ulrich et al. | 2011
- 3367
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Synthesis and evaluation of indole-based new scaffolds for antimicrobial activities—Identification of promising candidatesSingh, Palwinder / Verma, Puja / Yadav, Bhawna / Komath, Sneha S. et al. | 2011
- 3373
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Novel 12-membered non-antibiotic macrolides from erythromycin A; EM900 series as novel leads for anti-inflammatory and/or immunomodulatory agentsSugawara, Akihiro / Sueki, Akito / Hirose, Tomoyasu / Nagai, Kenichiro / Gouda, Hiroaki / Hirono, Shuichi / Shima, Hideaki / Akagawa, Kiyoko S. / Ōmura, Satoshi / Sunazuka, Toshiaki et al. | 2011
- 3377
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Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivativesChai, Yun / Wang, Jian / Liu, Mingliang / Yi, Hong / Sun, Lanying / You, Xuefu / Guo, Huiyuan et al. | 2011
- 3381
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Synthesis and anti-tumor activity of novel ethyl 3-aryl-4-oxo-3,3a,4,6-tetrahydro-1H-furo[3,4-c]pyran-3a-carboxylatesWang, Tiantian / Liu, Jia / Zhong, Hanyu / Chen, Huan / Lv, Zhiliang / Zhang, Yikai / Zhang, Mingfeng / Geng, Dongping / Niu, Chunjuan / Li, Yongmei et al. | 2011
- 3384
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3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammationChen, Jian Jeffrey / Nguyen, Thomas / D’Amico, Derin C. / Qian, Wenyuan / Human, Jason / Aya, Toshihiro / Biswas, Kaustav / Fotsch, Christopher / Han, Nianhe / Liu, Qingyian et al. | 2011
- 3390
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3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonistsWalsh, Shawn P. / Severino, Alexandra / Zhou, Changyou / He, Jiafang / Liang, Gui-Bai / Tan, Carina P. / Cao, Jin / Eiermann, George J. / Xu, Ling / Salituro, Gino et al. | 2011
- 3395
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Two methionine aminopeptidases from Acinetobacter baumannii are functional enzymesYuan, Hai / Chai, Sergio C. / Lam, Christopher K. / Howard Xu, H. / Ye, Qi-Zhuang et al. | 2011
- 3399
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2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activityBrown, Dean G. / Maier, Donna L. / Sylvester, Mark A. / Hoerter, Tiffany N. / Menhaji-Klotz, Elnaz / Lasota, Celina C. / Hirata, Lee T. / Wilkins, Deidre E. / Scott, Clay W. / Trivedi, Shephali et al. | 2011
- 3404
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Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitorsGlossop, Melanie S. / Bazin, Richard J. / Dack, Kevin N. / Fox, David N.A. / MacDonald, Graeme A. / Mills, Mark / Owen, Dafydd R. / Phillips, Chris / Reeves, Keith A. / Ringer, Tracy J. et al. | 2011
- 3407
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Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotypeSams, Anette Graven / Mikkelsen, Gitte Kobberøe / Brodbeck, Robbin M. / Pu, Xiaosui / Ritzén, Andreas et al. | 2011
- 3411
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Macrocyclic lactams as potent Hsp90 inhibitors with excellent tumor exposure and extended biomarker activityZapf, Christoph W. / Bloom, Jonathan D. / McBean, Jamie L. / Dushin, Russell G. / Nittoli, Thomas / Otteng, Mercy / Ingalls, Charles / Golas, Jennifer M. / Liu, Hao / Lucas, Judy et al. | 2011
- 3417
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New antiplasmodial indole alkaloids from Hunteria zeylanicaNugroho, Alfarius E. / Sugai, Masatomo / Hirasawa, Yusuke / Hosoya, Takahiro / Awang, Khalijah / Hadi, A. Hamid A. / Ekasari, Wiwied / Widyawaruyanti, Aty / Morita, Hiroshi et al. | 2011
- 3420
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Synthesis and properties of triazole-linked RNAMutisya, Daniel / Selvam, Chelliah / Kennedy, Scott D. / Rozners, Eriks et al. | 2011
- 3423
-
Macrocyclic chelator assembled RGD multimers for tumor targetingZhang, Xiaofen / Liu, Hongguang / Miao, Zheng / Kimura, Richard / Fan, Feiyue / Cheng, Zhen et al. | 2011
- 3427
-
A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: The disclosure of a new antitumor pharmacophore in protoapigenone 1Yuan, Qianying / Liu, Ziwei / Xiong, Chaomei / Wu, Liqian / Wang, Jianping / Ruan, Jinlan et al. | 2011
- 3431
-
Synthesis and in vitro antimicrobial activities of new (cyano-NNO-azoxy)pyrazole derivativesBoschi, Donatella / Guglielmo, Stefano / Aiello, Stefania / Morace, Giulia / Borghi, Elisa / Fruttero, Roberta et al. | 2011
- 3435
-
Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligandsZheng, Pinguan / Lieberman, Brian P. / Choi, Seok Rye / Plöessl, Karl / Kung, Hank F. et al. | 2011
- 3439
-
Synthesis and bioactivity of new Finasteride conjugateShuang, Zhao / Jiazhen, Wu / Lijuan, Yang / Zhuo, Li / Dahai, Yu / Jinfeng, Li / Jing, Yu / Yongtao, Liang / En-si, Wang / Xuexun, Fang et al. | 2011
- 3443
-
Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT methodBhavsar, Dhairya / Trivedi, Jalpa / Parekh, Shrey / Savant, Mahesh / Thakrar, Shailesh / Bavishi, Abhay / Radadiya, Ashish / Vala, Hardevsinh / Lunagariya, Jignesh / Parmar, Manisha et al. | 2011
- 3447
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Synthesis and SAR study of tricyclic sulfones as γ-secretase inhibitors: C-6 and C-8 positionsSu, Jing / Tang, Haiqun / McKittrick, Brian A. / Xu, Ruo / Clader, John W. / Greenlee, William J. / Hyde, Lynn / Zhang, Lili et al. | 2011
- 3447
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Synthesis and SAR study of tricyclic sulfones as g-secretase inhibitors: C-6 and C-8 positionsSu, J. / Tang, H. / McKittrick, B. A. / Xu, R. / Clader, J. W. / Greenlee, W. J. / Hyde, L. / Zhang, L. et al. | 2011
- 3452
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3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective leadSoth, Michael / Abbot, Sarah / Abubakari, Allassan / Arora, Nidhi / Arzeno, Humberto / Billedeau, Roland / Dewdney, Nolan / Durkin, Kieran / Frauchiger, Sandra / Ghate, Manjiri et al. | 2011
- 3452
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3-Amino-pyrazolo[3,4-d]pyrimidines as p38a kinase inhibitors: Design and development to a highly selective leadSoth, M. / Abbot, S. / Abubakari, A. / Arora, N. / Arzeno, H. / Billedeau, R. / Dewdney, N. / Durkin, K. / Frauchiger, S. / Ghate, M. et al. | 2011
- 3457
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Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonistsPrat, Maria / Buil, María Antonia / Fernández, Maria Dolors / Castro, Jordi / Monleón, Juan Manuel / Tort, Laia / Casals, Gaspar / Ferrer, Manuel / Huerta, Josep Maria / Espinosa, Sònia et al. | 2011
- 3462
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A new iridoid and effect on the rat aortic vascular smooth muscle cell proliferation of isolated compounds from Buddleja officinalisTai, Bui Huu / Nhiem, Nguyen Xuan / Quang, Tran Hong / Ngan, Nguyen Thi Thanh / Tung, Nguyen Huu / Kim, Yohan / Lee, Jung-Jin / Myung, Chang-Seon / Cuong, Nguyen Manh / Kim, Young Ho et al. | 2011
- 3467
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Design of a potent, soluble glucokinase activator with increased pharmacokinetic half-lifePike, Kurt G. / Allen, Joanne V. / Caulkett, Peter W.R. / Clarke, David S. / Donald, Craig S. / Fenwick, Mark L. / Johnson, Keith M. / Johnstone, Craig / McKerrecher, Darren / Rayner, John W. et al. | 2011
- 3471
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New indole amide derivatives as potent CRTH2 receptor antagonistsZaghdane, Helmi / Boyd, Michael / Colucci, John / Simard, Daniel / Berthelette, Carl / Leblanc, Yves / Wang, Zhaoyin / Houle, Robert / Lévesque, Jean François / Molinaro, Carmela et al. | 2011
- 3475
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Synthesis and antidyslipidemic activity of chalcone fibratesShukla, Poonam / Srivastava, Swayam P. / Srivastava, Rohit / Rawat, Arun K. / Srivastava, Arvind K. / Pratap, Ram et al. | 2011
- 3479
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Design, synthesis, and biological activity of novel Magmas inhibitorsJubinsky, Paul T. / Short, Mary K. / Ghanem, Mohmoud / Das, Bhaskar C. et al. | 2011
- 3483
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Anti-inflammatory activity of constituents from Glechoma hederacea var. longitubaKim, JinPyo / Song, SeokBean / Lee, IkSoo / Kim, YoungHo / Yoo, IckDong / Ryoo, InJa / Bae, KiHwan et al. | 2011
- 3488
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Non-oxime pyrazole based inhibitors of B-Raf kinaseNewhouse, Bradley J. / Hansen, Joshua D. / Grina, Jonas / Welch, Mike / Topalov, George / Littman, Nicole / Callejo, Michele / Martinson, Matthew / Galbraith, Sarah / Laird, Ellen R. et al. | 2010
- IFC
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Editorial board| 2011