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J Med Chem. 2014 Nov 13;57(21):9124-9. doi: 10.1021/jm501107q. Epub 2014 Nov 4.

Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990.

Author information

1
Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 5300 Chiron Way, Emeryville, California 94608, United States.

Abstract

Utilizing structure-based drug design, a novel dihydropyridopyrimidinone series which exhibited potent Hsp90 inhibition, good pharmacokinetics upon oral administration, and an excellent pharmacokinetic/pharmacodynamic relationship in vivo was developed from a commercial hit. The exploration of this series led to the selection of NVP-HSP990 as a development candidate.

PMID:
25368984
DOI:
10.1021/jm501107q
[Indexed for MEDLINE]

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