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77956133511
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note
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IR inhibition would induce diabetes in treated patients sooner or later, what is not compatible with the strategy to deal with cancer as with blood preasure in a live long medication context.
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19
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Munshi, S.; Kornienko, M.; Hall, D. L.; Reid, J. C.; Waxman, L.; Stirdivant, S. M.; Darke, P. L.; Kuo, L. C. Crystal structure of the apo, unactivated insulin-like growth factor-1 receptor kinase. Implication for inhibitor specificity J. Biol. Chem. 2002, 277, 38797-38802
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Synthesis and structure?activity relationship in a class of indolebutylpiperazines as dual 5-HT1A receptor agonists and serotonin reuptake inhibitors
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Heinrich, T.; Boettcher, H.; Gericke, R.; Bartoszyk, G. D.; Anzali, S.; Seyfried, C. A.; Greiner, H. E.; van Amsterdam, C. Synthesis and structure?activity relationship in a class of indolebutylpiperazines as dual 5-HT1A receptor agonists and serotonin reuptake inhibitors J. Med. Chem. 2004, 47, 4684-4692
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77956134059
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note
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A lot of different derivatives with modified indole cores and butyl chains were prepared. Unfortunately, all of these derivatizations did not result in any improvement, so we decided not to show these compounds explicitly.
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25
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77956161333
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DE 10102944
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Crassier, H.; Boettcher, H.; Eckert, U.; Bathe, A.; Emmert, S. Procedure for the production of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenylethyl)piperazin- 1-yl]methanone and its salts. DE 10102944, 2002.
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Procedure for the Production of (3-cyano-1H-indol-7-yl)-[4-(4- fluorophenylethyl)piperazin-1-yl]methanone and Its Salts
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Crassier, H.1
Boettcher, H.2
Eckert, U.3
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Emmert, S.5
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26
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77956162949
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See the Supporting Information
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See the Supporting Information.
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27
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0141925483
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Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 Å resolution
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Munshi, S.; Hall, D. L.; Kornienko, M.; Darke, P. L.; Kuo, L. C. Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 Å resolution Acta Crystallogr., Sect. D: Biol. Crystallogr. 2003, D59, 1725-1730
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33846607237
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Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor i (IGF-1R) kinase
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Wittman, M. D.; Balasubramanian, B.; Stoffan, K.; Velaparthi, U.; Liu, P.; Krishnanathan, S.; Carboni, J.; Li, A.; Greer, A.; Attar, R.; Gottardis, M.; Chang, C.; Jacobson, B.; Sun, Y.; Hansel, S.; Zoeckler, M.; Vyas, D. M. Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase Bioorg. Med. Chem. Lett. 2007, 17, 974-977
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14644433735
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The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy
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Warshamana-Greene, G. S.; Litz, J.; Buchdunger, E.; Garcia-Echeverria, C.; Hofmann, F.; Krystal, G. W. The insulin-like growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy Clin. Cancer Res. 2005, 11, 1563-1571
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Krystal, G.W.6
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30
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77956154744
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Unpublished results
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Unpublished results.
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