Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors (English)
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In:
Bioorganic and Medicinal Chemistry Letters
;
19
, 1
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21-26
;
2008
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ISSN:
- Article (Journal) / Electronic Resource
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Title:Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors
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Contributors:Stevens, Kirk L. ( author ) / Alligood, Krystal J. ( author ) / Alberti, Jennifer G. Badiang ( author ) / Caferro, Thomas R. ( author ) / Chamberlain, Stanley D. ( author ) / Dickerson, Scott H. ( author ) / Dickson, Hamilton D. ( author ) / Emerson, Holly K. ( author ) / Griffin, Robert J. ( author ) / Hubbard, Robert D. ( author )
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Published in:Bioorganic and Medicinal Chemistry Letters ; 19, 1 ; 21-26
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Publisher:
- New search for: Elsevier Ltd
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Publication date:2008-11-10
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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 19, Issue 1
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.
- 1
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Graphical contents list| 2008
- 17
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Identification of a small molecule β-secretase inhibitor that binds without catalytic aspartate engagementSteele, Thomas G. / Hills, Ivory D. / Nomland, Ashley A. / de León, Pablo / Allison, Timothy / McGaughey, Georgia / Colussi, Dennis / Tugusheva, Katherine / Haugabook, Sharie J. / Espeseth, Amy S. et al. | 2008
- 17
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Identification of a small molecule b-secretase inhibitor that binds without catalytic aspartate engagementSteele, T. G. / Hills, I. D. / Nomland, A. A. / de Leon, P. / Allison, T. / McGaughey, G. / Colussi, D. / Tugusheva, K. / Haugabook, S. J. / Espeseth, A. S. et al. | 2009
- 21
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Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitorsStevens, Kirk L. / Alligood, Krystal J. / Alberti, Jennifer G. Badiang / Caferro, Thomas R. / Chamberlain, Stanley D. / Dickerson, Scott H. / Dickson, Hamilton D. / Emerson, Holly K. / Griffin, Robert J. / Hubbard, Robert D. et al. | 2008
- 27
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Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitorsGoodman, Krista B. / Bury, Michael J. / Cheung, Mui / Cichy-Knight, Maria A. / Dowdell, Sarah E. / Dunn, Allison K. / Lee, Dennis / Lieby, Jeffrey A. / Moore, Michael L. / Scherzer, Daryl A. et al. | 2008
- 31
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Discovery of α-amidosulfones as potent and selective agonists of CB2: Synthesis, SAR, and pharmacokinetic propertiesMarx, Isaac E. / DiMauro, Erin F. / Cheng, Alan / Emkey, Renee / Hitchcock, Stephen A. / Huang, Liyue / Huang, Ming Y. / Human, Jason / Lee, Josie H. / Li, Xingwen et al. | 2008
- 31
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Discovery of a-amidosulfones as potent and selective agonists of CB2: Synthesis, SAR, and pharmacokinetic propertiesMarx, I. E. / DiMauro, E. F. / Cheng, A. / Emkey, R. / Hitchcock, S. A. / Huang, L. / Huang, M. Y. / Human, J. / Lee, J. H. / Li, X. et al. | 2009
- 36
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PEG-immobilization of cardol and soluble polymer-supported synthesis of some cardol–coumarin derivatives: Preliminary evaluation of their inhibitory activity on mushroom tyrosinaseTocco, Graziella / Fais, Antonella / Meli, Gabriele / Begala, Michela / Podda, Gianni / Fadda, M.Benedetta / Corda, Marcella / Attanasi, Orazio A. / Filippone, Paolino / Berretta, Stefano et al. | 2008
- 40
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Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonistsLebsack, Alec D. / Branstetter, Bryan J. / Hack, Michael D. / Xiao, Wei / Peterson, Matthew L. / Nasser, Nadia / Maher, Michael P. / Ao, Hong / Bhattacharya, Anindya / Kansagara, Mena et al. | 2008
- 47
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Calculation of binding free energies for non-zinc chelating pyrimidine dicarboxamide inhibitors with MMP-13Carrascal, Noel / Rizzo, Robert C. et al. | 2008
- 51
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Synthesis and neuropharmacological evaluation of esters of R(−)-N-alkyl-11-hydroxy-2-methoxynoraporphinesSi, Yu-Gui / Choi, Yong-Kee / Gardner, Matthew P. / Tarazi, Frank I. / Baldessarini, Ross J. / Neumeyer, John L. et al. | 2008
- 54
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Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitorsGuo, Zhuyan / Orth, Peter / Wong, Shing-Chun / Lavey, Brian J. / Shih, Neng-Yang / Niu, Xiaoda / Lundell, Daniel J. / Madison, Vincent / Kozlowski, Joseph A. et al. | 2008
- 58
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1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitorsManning, James R. / Sexton, Tammy / Childers, Steven R. / Davies, Huw M.L. et al. | 2008
- 62
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Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatmentMiller, Lori M. / Mayer, Scott C. / Berger, Dan M. / Boschelli, Diane H. / Boschelli, Frank / Di, Li / Du, Xuemei / Dutia, Minu / Floyd, Middleton B. / Johnson, Mark et al. | 2008
- 67
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Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitorsSteinmetzer, Torsten / Dönnecke, Daniel / Korsonewski, Martin / Neuwirth, Claudia / Steinmetzer, Peter / Schulze, Alexander / Saupe, Sebastian Martin / Schweinitz, Andrea et al. | 2008
- 74
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Synthesis of biflavones having a 6-O-7’’ linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthaseChe, Haiyan / Park, Byung Kyu / Lim, Hyun / Kim, Hyun Pyo / Chang, Hyeun Wook / Jeong, Jin-Hyun / Park, Haeil et al. | 2008
- 77
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Multifidone: A novel cytotoxic lathyrane-type diterpene having an unusual six-membered A ring from Jatropha multifidaDas, Biswanath / Reddy, Kongara Ravinder / Ravikanth, Bommena / Raju, Tuniki Venugopal / Sridhar, Balasubramanian / Khan, Patan Usman / Rao, Janapala Venkateswara et al. | 2008
- 80
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Synthesis and evaluation of novel photoreactive a-amino acid analog carrying acidic and cleavable functionsBongo, N. B. / Tomohiro, T. / Hatanaka, Y. et al. | 2009
- 80
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Synthesis and evaluation of novel photoreactive α-amino acid analog carrying acidic and cleavable functionsBongo, Nlandu B. / Tomohiro, Takenori / Hatanaka, Yasumaru et al. | 2008
- 83
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Novel fluorinated pseudopeptides as proteasome inhibitorsFormicola, Lucia / Maréchal, Xavier / Basse, Nicolas / Bouvier-Durand, Michelle / Bonnet-Delpon, Danièle / Milcent, Thierry / Reboud-Ravaux, Michèle / Ongeri, Sandrine et al. | 2008
- 87
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Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists—Structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC)Hansen, Camilla P. / Jensen, Anders A. / Balle, Thomas / Bitsch-Jensen, Klaus / Hassan, Mohamud M. / Liljefors, Tommy / Frølund, Bente et al. | 2008
- 92
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Design, synthesis, and biological evaluation of biotin-labeled (−)-ternatin, a potent fat-accumulation inhibitor against 3T3-L1 adipocytesShimokawa, Kenichiro / Yamada, Kaoru / Ohno, Osamu / Oba, Yuichi / Uemura, Daisuke et al. | 2008
- 96
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Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacerDhar, T.G. Murali / Yang, Guchen / Davies, Paul / Malley, Mary F. / Gougoutas, Jack Z. / Wu, Dauh-Rurng / Barrish, Joel C. / Carter, Percy H. et al. | 2008
- 100
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Efficient nucleic acid transduction with lipoplexes containing novel piperazine- and polyamine-conjugated cholesterol derivativesIslam, Rafique Ul / Hean, Justin / van Otterlo, Willem A.L. / de Koning, Charles B. / Arbuthnot, Patrick et al. | 2008
- 104
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11-Phenyl-[b,e]-dibenzazepine compounds: Novel antitumor agentsAl-Qawasmeh, Raed A. / Lee, Yoon / Cao, Ming-Yu / Gu, Xiaoping / Viau, Stéphane / Lightfoot, Jeff / Wright, Jim A. / Young, Aiping H. et al. | 2008
- 108
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Analogs of methyl-piperidinopyrazole (MPP): Antiestrogens with estrogen receptor α selective activityZhou, Hai-Bing / Carlson, Kathryn E. / Stossi, Fabio / Katzenellenbogen, Benita S. / Katzenellenbogen, John A. et al. | 2008
- 108
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Analogs of methyl-piperidinopyrazole (MPP): Antiestrogens with estrogen receptor a selective activityZhou, H. B. / Carlson, K. E. / Stossi, F. / Katzenellenbogen, B. S. / Katzenellenbogen, J. A. et al. | 2009
- 111
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Synthesis of a fluorescent 2′3′-dideoxycytosine analog, tCddPorterfield, William / Tahmassebi, Deborah C. et al. | 2008
- 111
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Synthesis of a fluorescent 2prime3prime-dideoxycytosine analog, tCddPorterfield, W. / Tahmassebi, D. C. et al. | 2009
- 114
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Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonistsWang, Yonghui / Busch-Petersen, Jakob / Wang, Feng / Kiesow, Terence J. / Graybill, Todd L. / Jin, Jian / Yang, Zheng / Foley, James J. / Hunsberger, Gerald E. / Schmidt, Dulcie B. et al. | 2008
- 119
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Sulfonamido-aryl ethers as bradykinin B1 receptor antagonistsCole, Andrew G. / Metzger, Axel / Brescia, Marc-Raleigh / Qin, Lan-Ying / Appell, Kenneth C. / Brain, Christopher T. / Hallett, Allan / Ganju, Pam / Denholm, Alastair A. / Wareing, James R. et al. | 2008
- 123
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3,4-Disubstituted indole acylsulfonamides: A novel series of potent and selective human EP3 receptor antagonistsZhou, Nian / Zeller, Wayne / Krohn, Michael / Anderson, Herb / Zhang, Jun / Onua, Emmanuel / Kiselyov, Alex S. / Ramirez, Jose / Halldorsdottir, Guðrún / Andrésson, Þorkell et al. | 2008
- 127
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3D-QSAR and QSSR studies of 3,8-diazabicyclo[4.2.0]octane derivatives as neuronal nicotinic acetylcholine receptors by comparative molecular field analysis (CoMFA)Ye, Mao / Dawson, Marcia I. et al. | 2008
- 132
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Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (−)-kaitocephalinVaswani, Rishi G. / Limon, Agenor / Reyes-Ruiz, Jorge Mauricio / Miledi, Ricardo / Chamberlin, A. Richard et al. | 2008
- 136
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One-pot synthesis of 5-phenylimino, 5-thieno or 5-oxo-1,2,3-dithiazoles and evaluation of their antimicrobial and antitumor activityKonstantinova, Lidia S. / Bol’shakov, Oleg I. / Obruchnikova, Natalia V. / Laborie, Hélène / Tanga, Annabelle / Sopéna, Valérie / Lanneluc, Isabelle / Picot, Laurent / Sablé, Sophie / Thiéry, Valérie et al. | 2008
- 142
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Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonistsKim, Jong Yup / Seo, Hee Jeong / Lee, Sung-Han / Jung, Myung Eun / Ahn, Kwangwoo / Kim, Jeongmin / Lee, Jinhwa et al. | 2008
- 146
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Synthesis and antifungal activity of 1H-pyrrolo[3,2-g]quinoline-4,9-diones and 4,9-dioxo-4,9-dihydro-1H-benzo[f]indolesRyu, Chung-Kyu / Lee, Jung Yoon / Jeong, Seong Hee / Nho, Ji-Hee et al. | 2008
- 149
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A model ternary heparin conjugate by direct covalent bond strategy applied to drug delivery systemWang, Ying / Xin, Dingcheng / Hu, Jiawen / Liu, Kaijian / Pan, Jiangao / Xiang, Jiannan et al. | 2008
- 153
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Synthesis and biological evaluation of new glutamic acid-based inhibitors of MurD ligaseTomašić, Tihomir / Zidar, Nace / Rupnik, Veronika / Kovač, Andreja / Blanot, Didier / Gobec, Stanislav / Kikelj, Danijel / Mašič, Lucija Peterlin et al. | 2008
- 158
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Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonistsBarnett, Heather A. / Coe, Diane M. / Cooper, Tony W.J. / Jack, Torquil I. / Jones, Haydn T. / Macdonald, Simon J.F. / McLay, Iain M. / Rayner, Natalie / Sasse, Rosemary Z. / Shipley, Tracy J. et al. | 2008
- 163
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Inhibition of purple acid phosphatase with α-alkoxynaphthylmethylphosphonic acidsMcGeary, Ross P. / Vella, Peter / Mak, Jeffrey Y.W. / Guddat, Luke W. / Schenk, Gerhard et al. | 2008
- 163
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Inhibition of purple acid phosphatase with a-alkoxynaphthylmethylphosphonic acidsMcGeary, R. P. / Vella, P. / Mak, J. Y. / Guddat, L. W. / Schenk, G. et al. | 2009
- 167
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Synthesis and biological evaluation of a series of tangeretin-derived chalconesQuintin, Jérôme / Desrivot, Julie / Thoret, Sylviane / Menez, Patrick Le / Cresteil, Thierry / Lewin, Guy et al. | 2008
- 170
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Pleuromutilin derivatives having a purine ring. Part 2: Influence of the central spacer on the antibacterial activity against Gram-positive pathogensHirokawa, Yoshimi / Kinoshita, Hironori / Tanaka, Tomoyuki / Nakamura, Takanori / Fujimoto, Koichi / Kashimoto, Shigeki / Kojima, Tsuyoshi / Kato, Shiro et al. | 2008
- 175
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Pleuromutilin derivatives having a purine ring. Part 3: Synthesis and antibacterial activity of novel compounds possessing a piperazine ring spacerHirokawa, Yoshimi / Kinoshita, Hironori / Tanaka, Tomoyuki / Nakamura, Takanori / Fujimoto, Koichi / Kashimoto, Shigeki / Kojima, Tsuyoshi / Kato, Shiro et al. | 2008
- 180
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Potent inhibitors of HCV-NS3 protease derived from boronic acidsVenkatraman, Srikanth / Wu, Wanli / Prongay, Andrew / Girijavallabhan, Viyyoor / George Njoroge, F. et al. | 2008
- 184
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Design, synthesis, and pharmacological and pharmacokinetic evaluation of 3-phenyl-5-pyridyl-1,2,4-triazole derivatives as xanthine oxidoreductase inhibitorsSato, Takahiro / Ashizawa, Naoki / Iwanaga, Takashi / Nakamura, Hiroshi / Matsumoto, Koji / Inoue, Tsutomu / Nagata, Osamu et al. | 2008
- 188
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Synthesis of tyrosinase inhibitory (4-oxo-4H-pyran-2-yl)acrylic acid ester derivativesKang, Soo Sung / Kim, Hyoung Ja / Jin, Changbae / Lee, Yong Sup et al. | 2008
- 192
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Two new cytotoxic diterpenes from the rhizomes of Hedychium spicatumReddy, P. Prabhakar / Rao, R. Ranga / Rekha, K. / Suresh Babu, K. / Shashidhar, J. / Shashikiran, G. / Vijaya Lakshmi, V. / Rao, J. Madhusudana et al. | 2008
- 196
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N,N-Dichloroaminosulfonic acids as novel topical antimicrobial agentsLow, Eddy / Nair, Satheesh / Shiau, Timothy / Belisle, Barbara / Debabov, Dmitri / Celeri, Chris / Zuck, Meghan / Najafi, Ron / Georgopapadakou, Nafsika / Jain, Rakesh et al. | 2008
- 199
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Synthesis and structure–activity relationships of oxamyl dipeptide caspase inhibitors developed for the treatment of liver diseaseUeno, Hirokazu / Kawai, Makoto / Shimokawa, Hirohisa / Hirota, Masako / Ohmi, Masashi / Sudo, Rie / Ohta, Atsuko / Arano, Yoshimasa / Hattori, Kazunari / Ohmi, Takashi et al. | 2008
- 203
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Syntheses and opioid receptor binding properties of carboxamido-substituted opioidsWentland, Mark P. / Lou, Rongliang / Lu, Qun / Bu, Yigong / VanAlstine, Melissa A. / Cohen, Dana J. / Bidlack, Jean M. et al. | 2008
- 209
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Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonistYang, Hanbiao / Lin, Xiao-Fa / Padilla, Fernando / Gabriel, Stephen D. / Heilek, Gabrielle / Ji, Changhua / Sankuratri, Surya / deRosier, André / Berry, Pamela / Rotstein, David M. et al. | 2008
- 214
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The discovery of highly potent CGRP receptor antagonistsStump, Craig A. / Bell, Ian M. / Bednar, Rodney A. / Bruno, Joseph G. / Fay, John F. / Gallicchio, Steven N. / Johnston, Victor K. / Moore, Eric L. / Mosser, Scott D. / Quigley, Amy G. et al. | 2008
- 218
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Biologically relevant chemical properties of peroxymonophosphate (O3POOH)LaButti, Jason N. / Gates, Kent S. et al. | 2008
- 222
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Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP)Sidique, Shyama / Ardecky, Robert / Su, Ying / Narisawa, Sonoko / Brown, Brock / Millán, José Luis / Sergienko, Eduard / Cosford, Nicholas D.P. et al. | 2008
- 226
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Beyond the MEK-pocket: Can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?Tecle, Haile / Shao, Jianxing / Li, Yanhong / Kothe, Michael / Kazmirski, Steven / Penzotti, Julie / Ding, Yuan-Hua / Ohren, Jeffrey / Moshinsky, Deb / Coli, Rocco et al. | 2008
- 230
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Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitorsPorter, John / Payne, Andrew / de Candole, Ben / Ford, Daniel / Hutchinson, Brian / Trevitt, Graham / Turner, James / Edwards, Chloe / Watkins, Clare / Whitcombe, Ian et al. | 2008
- 234
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TRAIL-enhancing activity of Erythrinan alkaloids from Erythrina velutinaOzawa, Masaaki / Etoh, Tadahiro / Hayashi, Masahiko / Komiyama, Kanki / Kishida, Akio / Ohsaki, Ayumi et al. | 2008
- 237
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Alcohol dehydrogenase-catalyzed in vitro oxidation of anandamide to N-arachidonoyl glycine, a lipid mediator: Synthesis of N-acyl glycinalsAneetha, Halikhedkar / O’Dell, David K. / Tan, Bo / Walker, J. Michael / Hurley, Thomas D. et al. | 2008
- 242
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2,6,9-Trisubstituted purine derivatives as protein A mimetics for the treatment of autoimmune diseasesZacharie, Boulos / Fortin, Daniel / Wilb, Nicole / Bienvenu, Jean-François / Asselin, Michel / Grouix, Brigitte / Penney, Christopher et al. | 2008
- 247
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Oxadiazolone bioisosteres of pregabalin and gabapentinWustrow, David J. / Belliotti, Thomas R. / Capiris, Thomas / Kneen, Clare O. / Bryans, Justin S. / Field, Mark J. / Williams, Dic / El-Kattan, Ayman / Buchholz, Lisa / Kinsora, Jack J. et al. | 2008
- 251
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Molecular modeling of the α9α10 nicotinic acetylcholine receptor subtypePérez, Edwin G. / Cassels, Bruce K. / Zapata-Torres, Gerald et al. | 2008
- 251
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Molecular modeling of the a9a10 nicotinic acetylcholine receptor subtypePerez, E. G. / Cassels, B. K. / Zapata-Torres, G. et al. | 2009
- 255
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Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamideRathish, I.G. / Javed, Kalim / Ahmad, Shamim / Bano, Sameena / Alam, M.S. / Pillai, K.K. / Singh, Surender / Bagchi, Vivek et al. | 2008
- 259
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Pyridine-3-carboxamides as novel CB2 agonists for analgesiaMitchell, William L. / Giblin, Gerard M.P. / Naylor, Alan / Eatherton, Andrew J. / Slingsby, Brian P. / Rawlings, Anthony D. / Jandu, Karamjit S. / Haslam, Carl P. / Brown, Andrew J. / Goldsmith, Paul et al. | 2008
- 264
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Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitorsChirapu, Srinivas Reddy / Pachaiyappan, Boobalan / Nural, Hikmet F. / Cheng, Xin / Yuan, Hongbin / Lankin, David C. / Abdul-Hay, Samer O. / Thatcher, Gregory R.J. / Shen, Yong / Kozikowski, Alan P. et al. | 2008
- 275
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Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activityXie, Fuchun / Zhao, Hongbing / Zhao, Lizhi / Lou, Liguang / Hu, Youhong et al. | 2008
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Fragment-based discovery of JAK-2 inhibitorsAntonysamy, Stephen / Hirst, Gavin / Park, Frances / Sprengeler, Paul / Stappenbeck, Frank / Steensma, Ruo / Wilson, Mark / Wong, Melissa et al. | 2008
- 283
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Corrigendum to “Synthesis of a 200-member library of squaric acid N-hydroxylamide amides” [Bioorg. Med. Chem. Lett. 18 (2008) 4968–4971]Charton, Julie / Leroux, Florence / Delaroche, Sylvain / Landry, Valérie / Déprez, Benoît P. / Déprez-Poulain, Rébecca F. et al. | 2008
- 284
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Corrigendum to “Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2” [Bioorg. Med. Chem. Lett. 18 (2008) 4267–4274]DiMauro, Erin F. / Buchanan, John L. / Chen, Alan / Emkey, Renee / Hitchcock, Stephen A. / Huang, Liyue / Huang, Ming Y. / Janosky, Brett / Lee, Josie H. / Li, Xingwen et al. | 2008
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Instructions to contributors| 2008
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Editorial board| 2008