Combining Hit Identification Strategies: Fragment-Based and in Silico Approaches to Orally Active 2-Aminothieno[2,3-d]pyrimidine Inhibitors of the Hsp90 Molecular Chaperone

Author:

Brough Paul A.1,Barril Xavier1,Borgognoni Jenifer1,Chene Patrick2,Davies Nicholas G. M.1,Davis Ben1,Drysdale Martin J.1,Dymock Brian1,Eccles Suzanne A.3,Garcia-Echeverria Carlos2,Fromont Christophe1,Hayes Angela3,Hubbard Roderick E.1,Jordan Allan M.1,Jensen Michael Rugaard2,Massey Andrew1,Merrett Angela1,Padfield Antony1,Parsons Rachel1,Radimerski Thomas2,Raynaud Florence I.3,Robertson Alan1,Roughley Stephen D.1,Schoepfer Joseph2,Simmonite Heather1,Sharp Swee Y.3,Surgenor Allan1,Valenti Melanie3,Walls Steven1,Webb Paul1,Wood Mike1,Workman Paul3,Wright Lisa1

Affiliation:

1. Vernalis Ltd., Granta Park, Great Abington, Cambridge CB21 6GB, U.K.

2. Novartis Institutes for Biomedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland

3. Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey SM2 5NG, U.K.

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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