期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 9, 页码 3368-3385出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200128m
关键词
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A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of structure-based design, parallel synthesis, and the application of medicinal chemistry principles. Through this process, the biochemical and cell-based potency of the original HTS lead were substantially improved along with the corresponding metabolic stability properties. These efforts culminated with the identification of a development candidate (compound 42) which displayed desired PK/PD relationships, significant efficacy in a melanoma A2058 xenograft tumor model, and attractive DMPK profiles.
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