4W7T | pdb_00004w7t

Design, Structure-Activity Relationship, and in Vivo Characterization of the Development Candidate NVP-HSP990.

McBride, C.M., Levine, B., Xia, Y., Bellamacina, C., Machajewski, T., Gao, Z., Renhowe, P., Antonios-McCrea, W., Barsanti, P., Brinner, K., Costales, A., Doughan, B., Lin, X., Louie, A., McKenna, M., Mendenhall, K., Poon, D., Rico, A., Wang, M., Williams, T.E., Abrams, T., Fong, S., Hendrickson, T., Lei, D., Lin, J., Menezes, D., Pryer, N., Taverna, P., Xu, Y., Zhou, Y., Shafer, C.M.

(2014) J Med Chem 57: 9124-9129

• PubMed: 25368984 Search on PubMed
• DOI: https://doi.org/10.1021/jm501107q
• Primary Citation of Related Structures:  
  4U93, 4W7T


• PubMed 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.

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Organizational Affiliation: 

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