The development of CNS-active LRRK2 inhibitors using property-directed optimisation

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 13, 2013, Pages 3690-3696

  Kavanagh, Madeline E ^a   Doddareddy, Munikumar Reddy ^b   Kassiou, Michael ^a,b  

^a UNIVERSITY OF SYDNEY   (Australia)

^b UNIVERSITY OF SYDNEY   (Australia)

Author keywords

CNS; GNE 7915; Kinase inhibitor; LRRK2; MPO Ligand efficiency; PARK8; Parkinson's disease; Structure property relationships

Indexed keywords

ADENOSINE TRIPHOSPHATE; ANAPLASTIC LYMPHOMA KINASE; ANILINOPYRIMIDINE DERIVATIVE; ANTINEOPLASTIC AGENT; CZC 25146; DIAZEPINONE DERIVATIVE; G 969; GNE 7915; GSK 2578215A; IMATINIB; LEUCINE RICH REPEAT KINASE 2; LEUCINE RICH REPEAT KINASE 2IN1; PYRAZOLOPYRIDINE DERIVATIVE; PYRIMIDINE DERIVATIVE; TAE 684; UNCLASSIFIED DRUG;

BINDING AFFINITY; BINDING SITE; BLOOD BRAIN BARRIER; CYTOTOXICITY; DRUG ACTIVITY; DRUG BINDING; DRUG PENETRATION; DRUG POTENCY; GENOTOXICITY; HIGH THROUGHPUT SCREENING; HUMAN GENOME; HYDROPHOBIC INTERACTION CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; LIPOPHILICITY; NEUROTOXICITY; NONHUMAN; PARKINSON DISEASE; PHYSICAL CHEMISTRY; PROTEIN DEPHOSPHORYLATION; REVIEW; STRUCTURE ACTIVITY RELATION;

CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MOLECULAR STRUCTURE; MORPHOLINES; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84878845602     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.04.086     Document Type: Review

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