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Developing a novel dual PI3K–mTOR inhibitor from the prodrug of a metabolite

This study presents a process of developing a novel PI3K–mTOR inhibitor through the prodrug of a metabolite. The lead compound (compound 1) was identified with similar efficacy as that of NVP-BEZ235 in a tumor xenograft model, but the exposure of compound 1 was much lower than that of NVP-BEZ235. Af...

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Detalles Bibliográficos
Autores principales: Zhou, Yan, Zhang, Genyan, Wang, Feng, Wang, Jin, Ding, Yanwei, Li, Xinyu, Shi, Chongtie, Li, Jiakui, Shih, Chengkon, You, Song
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Dove Medical Press 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5659256/
https://www.ncbi.nlm.nih.gov/pubmed/29118584
http://dx.doi.org/10.2147/OTT.S142492