Publisher: Elsevier

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Volume 13, Number 18, September 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. 2941-2949(9)

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A Perspective on Protein Kinase Inhibitors
pp. 2953-2953(1)
Author: Metz, W.A.

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Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-Bis anilino pyrimidines
pp. 2955-2960(6)
Authors: Beattie, J.F.; Breault, G.A.; Ellston, R.P.A.; Green, S.; Jewsbury, P.J.; Midgley, C.J.; Naven, R.T.; Minshull, C.A.; Pauptit, R.A.; Tucker, J.A.; Pease, J.E.

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Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines
pp. 2961-2966(6)
Authors: Breault, G.A.; Ellston, R.P.A.; Green, S.; James, S.R.; Jewsbury, P.J.; Midgley, C.J.; Pauptit, R.A.; Minshull, C.A.; Tucker, J.A.; Pease, J.E.

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Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching
pp. 2967-2971(5)
Authors: Furet, P.; Bold, G.; Hofmann, F.; Manley, P.; Meyer, T.; Altmann, K.

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Discovery and evaluation of 3-(5-Thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors
pp. 2973-2976(4)
Authors: Fraley, M.E.; Arrington, K.L.; Hambaugh, S.R.; Hoffman, W.F.; Cunningham, A.M.; Young, M.B.; Hungate, R.W.; Tebben, A.J.; Rutledge, R.Z.; Kendall, R.L.; Huckle, W.R.; McFall, R.C.; Coll, K.E.; Thomas, K.A.

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Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines
pp. 2977-2980(4)
Authors: Boschelli, D.H.; Powell, D.; Golas, J.M.; Boschelli, F.

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Anilinopyrazole as selective CDK2 inhibitors - design, synthesis, biological evaluation, and x-ray crystallographic analysis
pp. 2985-2988(4)
Authors: Tang, J.; Shewchuk, L.M.; Sato, H.; Hasegawa, M.; Washio, Y.; Nishigaki, N.

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Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors
pp. 2989-2992(4)
Authors: Moravcova, D.; Krystof, V.; Havlicek, L.; Moravec, J.V.; Lenobel, R.; Strnad, M.

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2,6,8,9-Tetrasubstituted Purines as New CDK1 Inhibitors
pp. 2993-2996(4)
Authors: Moravec, J.V.; Krystof, V.; Hanus, J.; Havlicek, L.; Moravcova, D.; Fuksova, K.; Kuzma, M.; Lenobel, R.; Otyepka, M.; Strnad, M.

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Combinatorial peptide microarrays for the rapid determination of kinase specificity
pp. 2997-3000(4)
Authors: Uttamchandani, M.; Chan, E.W.S.; Chen, G.Y.J.; Yao, S.Q.

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Acylsulfonamide-containing PTP1B inhibitors designed to mimic an enzyme-bound water of hydration
pp. 3005-3007(3)
Authors: Liu, D.; Gao, Y.; Voigt, J.H.; Lee, K.; Nicklaus, M.C.; Wu, L.; Zhang, Z.; Burke, T.R.

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Topological designing of 4-piperazinylquinazolines as antagonists of PDGFR tyrosine kinase family
pp. 3009-3014(6)
Authors: Khadikar, P.V.; Shrivastava, A.; Agrawal, V.K.; Srivastava, S.

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Synthesis and binding selectivity of 7- and 15-decylbenzolactone-V8 for the C1 domains of protein kinase C isozymes
pp. 3015-3019(5)
Authors: Nakagawa, Y.; Irie, K.; Yamanaka, N.; Ohigashi, H.; Tsuda, K.

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Imidazo[1,2-a]pyridines: A potent and selective class of cyclin-Dependent kinase inhibitors identified through structure-Based hybridisation
pp. 3021-3026(6)
Authors: Anderson, M.; Beattie, J.F.; Breault, G.A.; Breed, J.; Byth, K.F.; Culshaw, J.D.; Ellston, R.P.A.; Green, S.; Minshull, C.A.; Norman, R.A.; Pauptit, R.A.; Stanway, J.; Thomas, A.P.; Jewsbury, P.J.

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Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides
pp. 3027-3030(4)
Authors: Hernandez, A.; Balzarini, J.; Rodriguez-Barrios, F.; San-Felix, A.; Karlsson, A.; Gago, F.; Camarasa, M.; Perez-Perez, M.J.

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Synthesis and evaluation of 4-Anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade
pp. 3031-3034(4)
Authors: Berger, D.; Dutia, M.; Powell, D.; Wu, B.; Wissner, A.; Boschelli, D.H.; Floyd, M.B.; Zhang, N.; Torres, N.; Levin, J.; Du, X.; Wojciechowicz, D.; Discafani, C.; Kohler, C.; Kim, S.C.; Feldberg, L.R.; Collins, K.; Mallon, R.

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Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase
pp. 3035-3039(5)
Authors: Viht, K.; Padari, K.; Raidaru, G.; Subbi, J.; Tammiste, I.; Pooga, M.; Uri, A.

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Adenosine kinase inhibitors: polar 7-Substitutent of pyridopyrimidine derivatives improving their locomotor selectivity
pp. 3041-3044(4)
Authors: Zheng, G.Z.; Mao, Y.; Lee, C.; Pratt, J.K.; Koenig, J.R.; Perner, R.J.; Cowart, M.D.; Gfesser, G.A.; McGaraughty, S.; Chu, K.L.; Zhu, C.; Yu, H.; Kohlhaas, K.; Alexander, K.M.; Wismer, C.T.; Mikusa, J.; Jarvis, M.F.; Kowaluk, E.A.; Stewart, A.O.

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Thymidine and thymidine-5'-O-monophosphate analogues as inhibitors of Mycobacterium tuberculosis thymidylate kinase
pp. 3045-3048(4)
Authors: Vanheusden, V.; van Rompaey, P.; Munier-Lehmann, H.; Pochet, S.; Herdewijn, P.; van Calenbergh, S.

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Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3
pp. 3049-3053(5)
Authors: Zhang H.-C.; White, K.B.; Ye, H.; McComsey, D.F.; Derian, C.K.; Addo, M.F.; Andrade-Gordon, P.; Eckardt, A.J.; Conway, B.R.; Westover, L.; Xu, J.Z.; Look, R.; Demarest, K.T.; Emanuel, S.; Maryanoff, B.E.

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6-Aryl-pyrazolo[3,4-b]pyridines: potent inhibitors of glycogen synthase kinase-3 (GSK-3)
pp. 3055-3057(3)
Authors: Witherington, J.; Bordas, V.; Gaiba, A.; Garton, N.S.; Naylor, A.; Rawlings, A.D.; Slingsby, B.P.; Smith, D.G.; Takle, A.K.; Ward, R.W.

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6-Heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3)
pp. 3059-3062(4)
Authors: Witherington, J.; Bordas, V.; Gaiba, A.; Naylor, A.; Rawlings, A.D.; Slingsby, B.P.; Smith, D.G.; Takle, A.K.; Ward, R.W.

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Bone-Targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues
pp. 3063-3066(4)
Authors: Sundaramoorthi, R.; Shakespeare, W.C.; Keenan, T.P.; Metcalf, C.A.; Wang, Y.; Mani, U.; Taylor, M.; Liu, S.; Bohacek, R.S.; Narula, S.S.; Dalgarno, D.C.; van Schravandijk, M.R.; Violette, S.M.; Liou, S.; Adams, S.; Ram, M.K.; Keats, J.A.; Weigele, M.; Sawyer, T.K.

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Bone-Targeted 2,6,9-Trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases
pp. 3067-3070(4)
Authors: Wang, Y.; Metcalf, C.A.; Shakespeare, W.C.; Sundaramoorthi, R.; Keenan, T.P.; Bohacek, R.S.; van Schravendijk, M.R.; Violette, S.M.; Narula, S.S.; Dalgarno, D.C.; Haraldson, C.; Keats, J.; Liou, S.; Mani, U.; Pradeepan, S.; Ram, M.; Adams, S.; Weigele, M.; Sawyer, T.K.

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Bone-Targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents
pp. 3071-3074(4)
Authors: Vu, C.B.; Luke, G.P.; Kawahata, N.; Shakespeare, W.C.; Wang, Y.; Sundaramoorthi, R.; Metcalf, C.A.; Keenan, T.P.; Pradeepan, S.; Corpuz, E.; Merry, T.; Bohacek, R.S.; Dalgarno, D.C.; Narula, S.S.; van Schravendijk, M.R.; Ram, M.K.; Adams, S.; Liou, S.; Keats, J.A.; Violette, S.M.; Guan, W.; Weigele, M.; Sawyer, T.K.

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Design of quinolinedione-Based geldanamycin analogues
pp. 3075-3078(4)
Authors: Hargreaves, R.; David, C.L.; Whitesell, L.; Skibo, E.B.

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Structure-Based design of 2-Arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-Dependent kinases 1 and 2
pp. 3079-3082(4)
Authors: Sayle, K.L.; Bentley, J.; Boyle, F.T.; Calvert, A.H.; Cheng, Y.; Curtin, N.J.; Endicott, J.A.; Golding, B.T.; Hardcastle, I.R.; Jewsbury, P.; Mesguiche, V.; Newell, D.R.; Noble, M.E.M.; Parsons, R.J.; Pratt, D.J.; Wang, L.Z.; Griffin, R.J.

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2,6-Disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK)
pp. 3083-3086(4)
Authors: Hollick, J.J.; Golding, B.T.; Hardcastle, I.R.; Martin, N.; Richardson, C.; Rigoreau, L.J.M.; Smith, G.C.M.; Griffin, R.J.

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Indole-based heterocyclic inhibitors of p38α MAP kinase: designing a conformationally restricted analogue
pp. 3087-3090(4)
Authors: Mavunkel, B.J.; Chakravarty, S.; Perumattam, J.J.; Luedtke, G.R.; Liang, X.; Lim, D.; Xu, Y.; Laney, M.; Liu, D.Y.; Schreiner, G.F.; Lewicki, J.A.; Dugar, S.

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Potent quinoxaline-Based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR Exploration and Effective Bioisosteric Replacement of a phenyl substituent
pp. 3091-3095(5)
Authors: Myers, M.R.; He, W.; Hanney, B.; Setzer, N.; Maguire, M.P.; Zulli, A.; Bilder, G.; Galzcinski, H.; Amin, D.; Needle, S.; Spada, A.P.

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Potent quinoxaline-Based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor
pp. 3097-3100(4)
Authors: He, W.; Myers, M.R.; Hanney, B.; Spada, A.P.; Bilder, G.; Galzcinski, H.; Amin, D.; Needle, S.; Page, K.; Jayyosi, Z.; Perrone, M.H.

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The kinetics of binding to p38MAP kinase by analogues of BIRB 796
pp. 3101-3104(4)
Authors: Regan, J.; Pargellis, C.A.; Cirillo, P.F.; Gilmore, T.; Hickey, E.R.; Peet, G.W.; Proto, A.; Swinamer, A.; Moss, N.

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Mapping the kinase domain of janus kinase 3
pp. 3105-3110(6)
Authors: Adams, C.; Aldous, D.J.; Amendola, S.; Bamborough, P.; Bright, C.; Crowe, S.; Eastwood, P.; Fenton, G.; Foster, M.; Harrison, T.K.P.; King, S.; Lai, J.; Lawrence, C.; Letallec, J.; McCarthy, C.; Moorcroft, N.; Page, K.; Rao, S.; Redford, J.; Sadiq, S.; Smith, K.; Souness, J.E.; Thurairatnam, S.; Vine, M.; Wyman, B.

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Potent small molecule inhibitors of spleen tyrosine kinase (Syk)
pp. 3111-3114(4)
Authors: Lai, J.Y.Q.; Cox, P.J.; Patel, R.; Sadiq, S.; Aldous, D.J.; Thurairatnam, S.; Smith, K.; Wheeler, D.; Jagpal, S.; Parveen, S.; Fenton, G.; Harrison, T.K.P.; McCarthy, C.; Bamborough, P.

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