From on-target to off-target activity: Identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules

ChemMedChem

Volumn 8, Issue 7, 2013, Pages 1127-1137

  Woodland, Andrew ^a   Grimaldi, Raffaella ^a   Luksch, Torsten ^a   Cleghorn, Laura A T ^a   Ojo, Kayode K ^b   VanVoorhis, Wesley C ^b   Brenk, Ruth ^a   Frearson, Julie A ^a   Gilbert, Ian H ^a   Wyatt, Paul G ^a  

^a UNIVERSITY OF DUNDEE   (United Kingdom)

^b UNIVERSITY OF WASHINGTON SCHOOL OF MEDICINE   (United States)

Author keywords

Antiprotozoal agents; GSK3; Medicinal chemistry; Protein kinases; Trypanosoma brucei

Indexed keywords

(4 AMINO 2 ((2,6 DIMETHYLPHENYL)AMINO)THIAZOL 5 YL)(4 AMINO 2 ((2,6 DIMETH YL) (PHENYL)METHANONE; (4 AMINO 2 ((3,4 DIMETHYLPHENYL)AMINO)THIAZOL 5 YL) (PHENYL)METHANONE; (4 AMINO 2 ((CYCLOHEXYLMETHYL)AMINO)THIAZOL 5 YL) (PHENYL)METHANONE; (4 AMINO 2 (CYCLOHEXYLAMINO)THIAZOL 5 YL)(PHENYL)METHANONE; (4 AMINO 2 (PHENETHYLAMINO)THIAZOL 5 YL)(PHENYL)METHANONE; (4 AMINO 2 (PHENYLAMINO)THIAZOL 5 YL)(2,6 DIFLUOROPHENYL)METHANONE; (4 AMINO 2 (PHENYLAMINO)THIAZOL 5 YL)(2,6 DIMETHOXYPHENYL)METHANONE; (4 AMINO 2 (PHENYLAMINO)THIAZOL 5 YL)(3 BROMOPHENYL)METHANONE; 1 (4 AMINO 2 (CYCLOHEXYLAMINO)THIAZOL 5 YL) 2,2 DIMETHYLPROPAN 1 ONE); 4 AMINO 2 (PHENYLAMINO)THIAZOL 5 YL)(PHENYL)METHANONE; ANTIPROTOZOAL AGENT; BENZYL CARBAMIMIDOTHIOATE HYDROBROMIDE; GLYCOGEN SYNTHASE KINASE 3 INHIBITOR; THIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG BINDING; DRUG IDENTIFICATION; DRUG POTENCY; GENE LIBRARY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IN VITRO STUDY; NONHUMAN; PHARMACOPHORE; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; TRYPANOSOMA BRUCEI; VALIDATION PROCESS;

CELL LINE; CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; GLYCOGEN SYNTHASE KINASE 3; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PARASITIC SENSITIVITY TESTS; PROTEIN KINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI;

EID: 84879779739     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201300072     Document Type: Article

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