Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N- (piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas

Journal of Medicinal Chemistry

Volumn 55, Issue 11, 2012, Pages 5130-5142

  Oza, Vibha ^a   Ashwell, Susan ^a   Almeida, Lynsie ^a   Brassil, Patrick ^a   Breed, Jason ^a   Deng, Chun ^a   Gero, Thomas ^a   Grondine, Michael ^a   Horn, Candice ^a,d   Ioannidis, Stephanos ^a   Liu, Dongfang ^a,d   Lyne, Paul ^a   Newcombe, Nicholas ^a   Pass, Martin ^a   Read, Jon ^a   Ready, Shannon ^a,e   Rowsell, Siân ^a   Su, Mei ^a   Toader, Dorin ^a   Vasbinder, Melissa ^a   Yu, Dingwei ^a   Yu, Yan ^a   Xue, Yafeng ^b   Zabludoff, Sonya ^a,d   Janetka, James ^a,c   more..

^a ASTRAZENECA   (United Kingdom)

^b ASTRAZENECA R AND D   (Sweden)

^c WASHINGTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

^d Box 8231 ^*  (United States)

^e MEDIMMUNE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 (3 FLUOROPHENYL) N (3 PIPERIDINYL) 3 UREIDO 2 THIOPHENECARBOXAMIDE; CHECKPOINT KINASE 1; CHECKPOINT KINASE 2; I KAPPA B KINASE BETA; PROTEIN KINASE INHIBITOR; STRESS ACTIVATED PROTEIN KINASE; THIOPHENECARBOXAMIDE UREA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG POTENTIATION; DRUG SELECTIVITY; DRUG SOLUBILITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVATION; HUMAN; HUMAN CELL; HYDROGEN BOND; IN VIVO STUDY; ISOMERISM; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION; THERMODYNAMICS; X RAY CRYSTALLOGRAPHY;

EID: 84862282465     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm300025r     Document Type: Article

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