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Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990
Christopher M McBride1, Barry Levine, Yi Xia
1Global Discovery Chemistry/Oncology & Exploratory Chemistry, Novartis Institutes for Biomedical Research , 5300 Chiron Way, Emeryville, California 94608, United States.
Journal of Medicinal Chemistry
|November 5, 2014
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.

