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

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

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...

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Veröffentlicht in:Journal of medicinal chemistry 2014-11, Vol.57 (21), p.9124-9129
Hauptverfasser: McBride, Christopher M, Levine, Barry, Xia, Yi, Bellamacina, Cornelia, Machajewski, Timothy, Gao, Zhenhai, Renhowe, Paul, Antonios-McCrea, William, Barsanti, Paul, Brinner, Kristin, Costales, Abran, Doughan, Brandon, Lin, Xiaodong, Louie, Alicia, McKenna, Maureen, Mendenhall, Kris, Poon, Daniel, Rico, Alice, Wang, Michael, Williams, Teresa E, Abrams, Tinya, Fong, Susan, Hendrickson, Thomas, Lei, Dachuan, Lin, Julie, Menezes, Daniel, Pryer, Nancy, Taverna, Pietro, Xu, Yongjin, Zhou, Yasheen, Shafer, Cynthia M
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacokinetics
Antineoplastic Agents - pharmacology
HSP90 Heat-Shock Proteins - antagonists & inhibitors
Mice
Pyridones - chemical synthesis
Pyridones - pharmacokinetics
Pyridones - pharmacology
Pyrimidines - chemical synthesis
Pyrimidines - pharmacokinetics
Pyrimidines - pharmacology
Structure-Activity Relationship
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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm501107q