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Novel cinnoline-based inhibitors of LRRK2 kinase activity

Garofalo, AW and Adler, M and Aubele, DL and Bowers, S and Franzini, M and Goldbach, E and Lorentzen, C and Neitz, RJ and Probst, GD and Quinn, KP and Santiago, P and Sham, HL and Tam, D and Truong, AP and Ye, XM and Ren, Z (2013) Novel cinnoline-based inhibitors of LRRK2 kinase activity. Bioorganic and Medicinal Chemistry Letters. pp. 71-74.

Abstract

Leucine rich repeat kinase 2 (LRRK2) has been implicated in the pathogenesis of Parkinson's disease (PD). Inhibition of LRRK2 kinase activity is a therapeutic approach that may lead to new treatments for PD. Herein we report the discovery of a series of cinnoline-3-carboxamides that are potent against both wild-type and mutant LRRK2 kinase activity in biochemical assays. These compounds are also shown to be potent inhibitors in a cellular assay and to have good to excellent CNS penetration

Item Type: Article
Additional Information: pubid: 163 nvp_institute: NIBR contributor_address: (Garofalo, Aubele, Bowers, Franzini, Neitz, Probst, Sham, Truong, Ye) Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, United States (Adler) Department of Molecular Design, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, United States (Goldbach, Lorentzen, Quinn, Santiago) Department of Drug Metabolism and Pharmacokinetics, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, United States (Tam, Ren) Department of Assay Development, Elan Pharmaceuticals, 180 Oyster Point Blvd, South San Francisco, CA 94080, United States (Lorentzen) Novartis Institutes for Biomedical Research, Emeryville, CA 94608, United States (Neitz) Small Molecule Discovery Center, Univ. of California-San Francisco, San Francisco, CA 98158, United States
Date Deposited: 13 Oct 2015 13:12
Last Modified: 13 Oct 2015 13:12
URI: https://oak.novartis.com/id/eprint/21993

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