Fragment-based discovery of 7-azabenzimidazoles as potent, highly selective, and orally active CDK4/6 inhibitors

ACS Medicinal Chemistry Letters

Volumn 3, Issue 6, 2012, Pages 445-449

  Cho, Young Shin ^a   Angove, Hayley ^b   Brain, Christopher ^a   Chen, Christine Hiu Tung ^a   Cheng, Hong ^a   Cheng, Robert ^b   Chopra, Rajiv ^a   Chung, Kristy ^a   Congreve, Miles ^b   Dagostin, Claudio ^b   Davis, Deborah J ^b   Feltell, Ruth ^b   Giraldes, John ^a   Hiscock, Steven D ^b   Kim, Sunkyu ^a   Kovats, Steven ^a   Lagu, Bharat ^a   Lewry, Kim ^b   Loo, Alice ^a   Lu, Yipin ^a   Luzzio, Michael ^a   Maniara, Wiesia ^a   McMenamin, Rachel ^b   Mortenson, Paul N ^b   Benning, Rajdeep ^b   O'Reilly, Marc ^b   Rees, David C ^b   Shen, Junqing ^a   Smith, Troy ^a   Wang, Yaping ^a   Williams, Glyn ^b   Woolford, Alison J A ^b   Wrona, Wojciech ^a   Xu, Mei ^a   Yang, Fan ^a   Howard, Steven ^b   more..

^a NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^b ASTEX PHARMACEUTICALS   (United Kingdom)

Author keywords

CDK4 6; fragment based screening; mantle cell lymphoma; pRb phosphorylation; structure guided optimization

Indexed keywords

7 AZABENZIMIDAZOLE DERIVATIVE; CYCLIN DEPENDENT KINASE 4; CYCLIN DEPENDENT KINASE 6; IMIDAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; ARTICLE; DRUG MECHANISM; DRUG SCREENING; DRUG STRUCTURE; ENZYME ASSAY; ENZYME INHIBITION; IC 50; PRIORITY JOURNAL; X RAY CRYSTALLOGRAPHY;

EID: 84862285006     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml200241a     Document Type: Article

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