Imidazopyridazines as potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1): Preparation and evaluation of pyrazole linked analogues

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 21, 2013, Pages 6019-6024

  Large, Jonathan M ^a   Osborne, Simon A ^a   Smiljanic Hurley, Ela ^a   Ansell, Keith H ^a   Jones, Hayley M ^a   Taylor, Debra L ^a   Clough, Barbara ^b   Green, Judith L ^b   Holder, Anthony A ^b  

^a Centre for Therapeutics Discovery   (United Kingdom)

^b NATIONAL INSTITUTE FOR MEDICAL RESEARCH   (United Kingdom)

Author keywords

Calcium dependent protein kinase 1; Imidazopyridazine; Malaria; Plasmodium falciparum; SAR

Indexed keywords

ANTIMALARIAL AGENT; CALCIUM DEPENDENT PROTEIN KINASE 1; PROTEIN KINASE; PYRIDAZINE DERIVATIVE; UNCLASSIFIED DRUG;

ANTIMALARIAL ACTIVITY; ARTICLE; CONTROLLED STUDY; ENZYME INHIBITION; EVALUATION; IC 50; LIPOPHILICITY; NONHUMAN; PLASMODIUM FALCIPARUM; STRUCTURE ACTIVITY RELATION;

PLASMODIUM FALCIPARUM;

CALCIUM-DEPENDENT PROTEIN KINASE 1; IMIDAZOPYRIDAZINE; MALARIA; PLASMODIUM FALCIPARUM; SAR;

ANTIMALARIALS; HUMANS; MALARIA, FALCIPARUM; PLASMODIUM FALCIPARUM; PROTEIN KINASES; PROTOZOAN PROTEINS; PYRIDAZINES;

EID: 84885187477     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2013.08.010     Document Type: Article

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19. Kinase selectivity profiling was carried out by the National Centre for Protein Kinase Profiling at the MRC Protein Phosphorylation Unit (University of Dundee, UK).
20. Kinases inhibited by 12: PRK2, PKD1, MSK1, MNK1, SmMLCK, CHK1, CHK2, Aurora B, NUAK1, PIM1, GCK, MINK1, MLK1, MLK3, IRAK4, SRC, LCK, YES1, EPH-A2, FGF-R1, HER4, VEG-FR. By 27: RSK1, PRK2, CHK1, MELK, NUAK 1, PIM1, MST2, GCK, MINK1, MLK1, MLK3, IRAK4, SRC, LCK, CSK, YES1, BTK, EPH-A2, EPH-B3, HER4, VEG-FR. By 36: RSK1, ROCK2, PRK2, MNK1, MNK2, SmMLCK, PHK, CHK1, MARK3, BRSK2, MELK, NUAK1, CK1, CK2, DRYK1A, PIM1, PAK4, MST2, GCK, MINK1, MLK1, MLK3, IRAK4, SRC, YES1, BTK, EPH-A2, HER4, VEG-FR.