Discovery of novel 1,2,3,4-tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones as potent and selective inhibitors of KDR: synthesis, SAR, and pharmacokinetic properties |
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| Authors: | Choquette Deborah Teffera Yohannes Polverino Anthony Harmange Jean-Christophe |
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| Institution: | aDepartment of Medicinal Chemistry, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA;bDepartment of Pharmacokinetics and Drug Metabolism, Amgen Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA;cDepartment of Oncology, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA |
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| Abstract: | 1,2,3,4-Tetrahydroisoquinolines and 3,4-dihydroisoquinoline-1(2H)-ones were identified as potent and selective inhibitors of KDR. The discovery, synthesis, and structure–activity relationships of these novel inhibitors are reported. In vitro metabolism and pharmacokinetic profiles of the most interesting compounds are discussed. |
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| Keywords: | KDR VEGFR-2 1 2 3 4-Trahydroisoquinolines 3 4-Dihydroisoquinoline-1(2H)-ones |
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