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Publisher: Elsevier

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Volume 13, Number 4, February 2003

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Editorial Board
pp. CO2-CO2(1)

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Contents List
pp. iii

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Graphical Abstracts
pp. 587-596(10)

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Pyridazinones as selective cyclooxygenase-2 inhibitors
pp. 597-600(4)
Authors: Li, C.S.; Brideau, C.; Chan, C.C.; Savoie, C.; Claveau, D.; Charleson, S.; Gordon, R.; Greig, G.; Gauthier, J.Y.; Lau, C.K.; Riendeau, D.; Therien, M.; Wong, E.; Prasit, P.

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Synthesis of N,N',N''-trisubstituted thiourea derivatives and their antagonist effect on the vanilloid receptor
pp. 601-604(4)
Authors: Park, H.; Park, M.; Choi, J.; Choi, S.; Lee, J.; Park, B.; Kim, M.G.; Suh, Y.; Cho, H.; Oh, U.; Lee, J.; Kim, H.; Park, Y.; Koh, H.; Lim, K.M.; Moh, J.; Jew S.-s.

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Synthesis, antiviral activity and pharmacokinetics of P1/P1' substituted 3-aminoindazole cyclic urea HIV protease inhibitors
pp. 605-608(4)
Authors: Kaltenbach, R.F.; Patel, M.; Waltermire, R.E.; Harris, G.D.; Stone, B.R.P.; Klabe, R.M.; Garber, S.; Bacheler, L.T.; Cordova, B.C.; Logue, K.; Wright, M.R.; Erickson-Viitanen, S.; Trainor, G.L.

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Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities
pp. 609-612(4)
Authors: Jew S.-s.; Park, B.; Lim, D.; Kim, M.G.; Chung, I.K.; Kim, J.H.; Hong, C.I.; Kim, J.; Park, H.; Lee, J.; Park, H.

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Synthesis of non-Natural C2-Homo-ceramide and its apoptotic activity against HL-60 cells
pp. 613-616(4)
Authors: Shikata, K.; Niiro, H.; Azuma, H.; Tachibana, T.; Ogino, K.

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Enterolosaponins A and B, novel triterpene bisdesmosides from Enterolobium contortisiliquum, and evaluation for their macrophage-oriented cytotoxic activity
pp. 623-627(5)
Authors: Mimaki, Y.; Harada, H.; Sakuma, C.; Haraguchi, M.; Yui, S.; Kudo, T.; Yamazaki, M.; Sashida, Y.

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Synthesis of dopamine transporter selective 3-{2-(Diarylmethoxyethylidene)}-8-alkylaryl-8-azabicyclo[3.2.1]octanes
pp. 629-632(4)
Authors: Bradley, A.L.; Izenwasser, S.; Wade, D.; Cararas, S.; Trudell, M.L.

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Identification of a High-Affinity Phosphopeptide Inhibitor of Stat3
pp. 633-636(4)
Authors: Ren, Z.; Cabell, L.A.; Schaefer, T.S.; McMurray, J.S.

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Discovery and Biological Evaluation of Potent Dual ErbB-2/EGFR Tyrosine Kinase Inhibitors: 6-Thiazolylquinazolines
pp. 637-640(4)
Authors: Gaul, M.D.; Guo, Y.; Affleck, K.; Cockerill, G.S.; Gilmer, T.M.; Griffin, R.J.; Guntrip, S.; Keith, B.R.; Knight, W.B.; Mullin, R.J.; Murray, D.M.; Rusnak, D.W.; Smith, K.; Tadepalli, S.; Wood, E.R.; Lackey, K.

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Synthesis and preliminary biological evaluation of 6-O-[11C]-[(methoxymethyl)benzyl]guanines, new potential PET breast cancer imaging agents for the DNA repair protein AGT
pp. 641-644(4)
Authors: Liu, X.; Zheng Q.-H.; Fei, X.; Wang, J.; Ohannesian, D.W.; Erickson, L.C.; Stone, K.L.; Hutchins, G.D.

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Structure-Activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution
pp. 649-652(4)
Authors: Danho, W.; Swistok, J.; Wai-Hing Cheung, A.; Kurylko, G.; Franco, L.; Chu, X.; Chen, L.; Yagaloff, K.

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Protective effect of imidazolopyrazinone antioxidants on ischemia/reperfusion injury
pp. 653-656(4)
Authors: Arrault, A.; Dubuisson, M.; Gharbi, S.; Marchand, C.; Verbeuren, T.; Rupin, A.; Cordi, A.; Bouskela, E.; Rees, J.; Marchand-Brynaert, J.

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Design, synthesis and biological evaluation of benzimidazole/benzothiazole and benzoxazole derivatives as cyclooxygenase inhibitors
pp. 657-660(4)
Authors: Paramashivappa, R.; Phani Kumar, P.; Subba Rao, P.V.; Srinivasa Rao, A.

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Synthesis of fluorescence-Labeled sphingosine and sphingosine 1-phosphate; effective tools for sphingosine and sphingosine 1-phosphate behavior
pp. 661-664(4)
Authors: Hakogi, T.; Shigenari, T.; Katsumura, S.; Sano, T.; Kohno, T.; Igarashi, Y.

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Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-Positive antibacterial activity
pp. 665-668(4)
Authors: Jarvest, R.L.; Berge, J.M.; Brown, M.J.; Brown, P.; Elder, J.S.; Forrest, A.K.; Houge-Frydrych, C.S.V.; O'Hanlon, P.J.; McNair, D.J.; Rittenhouse, S.; Sheppard, R.J.

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Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir
pp. 669-673(5)
Authors: Masuda, T.; Shibuya, S.; Arai, M.; Yoshida, S.; Tomozawa, T.; Ohno, A.; Yamashita, M.; Honda, T.

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Ganglioside binding pattern of CD33-related siglecs
pp. 675-678(4)
Authors: Rapoport, E.; Mikhalyov, I.; Zhang, J.; Crocker, P.; Bovin, N.

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Exploring new non-sugar sulfated molecules as activators of antithrombin
pp. 679-683(5)
Authors: Gunnarsson, G.T.; Desai, U.R.

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Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists
pp. 693-696(4)
Authors: Curtis, N.R.; Diggle, H.J.; Kulagowski, J.J.; London, C.; Grimwood, S.; Hutson, P.H.; Murray, F.; Richards, P.; Macaulay, A.; Wafford, K.A.

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Orally Efficacious NR2B-Selective NMDA Receptor Antagonists
pp. 697-700(4)
Authors: Claiborne, C.F.; McCauley, J.A.; Libby, B.E.; Curtis, N.R.; Diggle, H.J.; Kulagowski, J.J.; Michelson, S.R.; Anderson, K.D.; Claremon, D.A.; Freidinger, R.M.; Bednar, R.A.; Mosser, S.D.; Gaul, S.L.; Connolly, T.M.; Condra, C.L.; Bednar, B.; Stump, G.L.; Lynch, J.J.; Macaulay, A.; Wafford, K.A.; Koblan, K.S.; Liverton, N.J.

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Design, synthesis, and discovery of 5-piperazinyl-1,2,6,7-tetrahydro-5H-azepino[3,2,1-hi]indol-4-one derivatives: A novel series of mixed dopamine D2/D4 receptor antagonist
pp. 701-704(4)
Authors: Zhao, H.; Zhang, X.; Hodgetts, K.; Thurkauf, A.; Hammer, J.; Chandrasekhar, J.; Kieltyka, A.; Brodbeck, R.; Rachwal, S.; Primus, R.; Manly, C.

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Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist
pp. 705-708(4)
Authors: Palani, A.; Shapiro, S.; Clader, J.W.; Greenlee, W.J.; Blythin, D.; Cox, K.; Wagner, N.E.; Strizki, J.; Baroudy, B.M.; Dan, N.

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Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides
pp. 709-712(4)
Authors: Palani, A.; Shapiro, S.; Clader, J.W.; Greenlee, W.J.; Vice, S.; McCombie, S.; Cox, K.; Strizki, J.; Baroudy, B.M.

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Four novel bis-(naphtho--pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase
pp. 713-717(5)
Authors: Singh, S.B.; Zink, D.L.; Bills, G.F.; Teran, A.; Silverman, K.C.; Lingham, R.B.; Felock, P.; Hazuda, D.J.

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A structure-Permeability study of small drug-like molecules
pp. 719-722(4)
Authors: Fichert, T.; Yazdanian, M.; Proudfoot, J.R.

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Design, synthesis, and structure-Activity relationships of unsubstituted piperazinone-Based transition state factor Xa inhibitors
pp. 723-728(6)
Authors: Huang, W.; Naughton, M.A.; Yang, H.; Su, T.; Dam, S.; Wong, P.W.; Arfsten, A.; Edwards, S.; Sinha, U.; Hollenbach, S.; Scarborough, R.M.; Zhu B.-Y.

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Design, synthesis, and structure-Activity relationships of substituted piperazinone-Based transition state factor Xa inhibitors
pp. 729-732(4)
Authors: Su, T.; Yang, H.; Volkots, D.; Woolfrey, J.; Dam, S.; Wong, P.; Sinha, U.; Scarborough, R.M.; Zhu B.-Y.

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Binding of nicotine and homoazanicotine analogues at neuronal nicotinic acetylcholinergic (nACh) receptors
pp. 733-735(3)
Authors: Ferretti, G.; Dukat, M.; Giannella, M.; Piergentili, A.; Pigini, M.; Quaglia, W.; Damaj, M.I.; Martin, B.R.; Glennon, R.A.

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Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors
pp. 741-744(4)
Authors: Cote, B.; Frenette, R.; Prescott, S.; Blouin, M.; Brideau, C.; Ducharme, Y.; Friesen, R.W.; Laliberte, F.; Masson, P.; Styhler, A.; Girard, Y.

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Lead discovery of α,-Unsaturated sulfones from a combinatorial library as inhibitors of inducible VCAM-1 expression
pp. 745-748(4)
Authors: Ni, L.; Zheng, X.S.; Somers, P.K.; Hoong, L.K.; Hill, R.R.; Marino, E.M.; Suen, K.; Saxena, U.; Meng, C.Q.

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1,4-Dibenzylpiperazines possess anticocaine activity
pp. 749-751(3)
Authors: Foster, A.; Wu, H.; Chen, W.; Williams, W.; Bowen, W.D.; Matsumoto, R.R.; Coop, A.

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Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists
pp. 753-756(4)
Authors: Matthews, J.M.; Greco, M.N.; Hecker, L.R.; Hoekstra, W.J.; Andrade-Gordon, P.; Garavilla, L.d.; Demarest, K.T.; Ericson, E.; Gunnet, J.W.; Hageman, W.; Look, R.; Moore, J.B.; Maryanoff, B.E.

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Cryptophycin affinity labels: synthesis and biological activity of a benzophenone analogue of cryptophycin-24
pp. 757-760(4)
Authors: Vidya, R.; Eggen, M.; Georg, G.I.; Himes, R.H.

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Synthesis and biological activities of novel -Carbolines as PDE5 inhibitors
pp. 761-765(5)
Authors: Sui, Z.; Guan, J.; Macielag, M.J.; Jiang, W.; Qiu, Y.; Kraft, P.; Bhattacharjee, S.; John, T.M.; Craig, E.; Haynes-Johnson, D.; Clancy, J.

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Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics
pp. 767-770(4)
Authors: Lee, T.; Robichaud, A.J.; Boyle, K.E.; Lu, Y.; Robertson, D.W.; Miller, K.J.; Fitzgerald, L.W.; McElroy, J.F.; Largent, B.L.

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