Discovery of 4-aryl-N-arylcarbonyl-2-aminothiazoles as Hec1/Nek2 inhibitors. Part I: Optimization of in vitro potencies and pharmacokinetic properties

Journal of Medicinal Chemistry

Volumn 57, Issue 10, 2014, Pages 4098-4110

  Lee, Ying Shuan E ^a   Chuang, Shih Hsien ^a   Huang, Lynn Y L ^b   Lai, Chun Liang ^a   Lin, Yu Hsiang ^a   Yang, Ju Ying ^a   Liu, Chia Wei ^a   Yang, Sheng Chuan ^a   Lin, Her Sheng ^a   Chang, Chia Chi ^b   Lai, Jun Yu ^c   Jian, Pei Shiou ^c   Lam, King ^a   Chang, Jia Ming ^a   Lau, Johnson Y N ^b   Huang, Jiann Jyh ^a,c  

^a DEVELOPMENT CENTER FOR BIOTECHNOLOGY   (Taiwan)

^b Taivex Therapeutics Corporation   (Taiwan)

^c NATIONAL CHIAYI UNIVERSITY   (Taiwan)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINOTHIAZOLE DERIVATIVE; 2 CHLORO N (4 MESITYLTHIAZOL 2 YL)ISONICOTINAMIDE; 2 CHLORO N [4 (4 METHOXY 2,6 DIMETHYLPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; 2 FLUORO N [4 (4 ISOPROPOXY 2,6 DIMETHYLPHENYL)THIAZOL 2YL]ISONICOTINAMIDE; 2 FLUORO N [4 (4 METHOXY 2,6 DIMETHYLPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; 2 FLUORO N [4 [4 (4 METHOXYPHENOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2 YL]ISONICOTINAM; 4 CYANO N (4 MESITYLTHIAZOL 2 YL)BENZAMIDE; 4 [(4 MESITYLTHIAZOL 2 YL)CARBAMOYL]PYRIDINE 1 OXIDE; ANTINEOPLASTIC AGENT; ASTEMIZOLE; N (4 MESITYLTHIAZOL 2 YL) 2 (PYRIDIN 4 YL)ACETAMIDE; N (4 MESITYLTHIAZOL 2 YL)ISONICOTINAMIDE; N [4 (2,6 DIFLUORO 4 METHOXYPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; N [4 (2,6 DIMETHYL 4 PHENOXYPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; N [4 (4 ISOBUTOXY 2,6 DIMETHYLPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; N [4 (4 ISOPROPOXY 2,6 DIMETHYLPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; N [4 (4 METHOXY 2,6 DIMETHYLPHENYL)THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [2,6 DIMETHYL 4 (4 TOLYLOXY)PHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [2,6 DIMETHYL 4 [4 (TRIFLUOROMETHYL)PHENOXY]PHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [4 (3 METHOXYPHENOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2YL]ISONICOTINAMIDE; N [4 [4 (3,5 DIMETHYLPHENOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [4 (4 ETHYLPHENOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [4 (4 FLUOROPHENOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [4 (4 METHOXYPHENOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2YL]ISONICOTINAMIDE; N [4 [4 (BENZO[D ][1,3]DIOXOL 5 YLOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; N [4 [4 (CYCLOPENTYLOXY) 2,6 DIMETHYLPHENYL]THIAZOL 2 YL]ISONICOTINAMIDE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; APOPTOSIS; AREA UNDER THE CURVE; ARTICLE; BINDING ASSAY; CANCER CELL LINE; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; DRUG TARGETING; IC 50; IN VITRO STUDY; IN VIVO STUDY; MITOSIS; MOUSE; NONHUMAN; PHENOTYPE; PROCESS OPTIMIZATION; RAT; STRUCTURE ACTIVITY RELATION; TUMOR XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; DRUG DISCOVERY; FEMALE; HUMANS; MALE; MICE; MICE, INBRED BALB C; NUCLEAR PROTEINS; PROTEIN-SERINE-THREONINE KINASES; RATS; RATS, SPRAGUE-DAWLEY; THIAZOLES; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84901268379     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401990s     Document Type: Article

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