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Lead optimization and efficacy evaluation of quinazoline-based BET family inhibitors for potential treatment of cancer and inflammatory diseases

Extensive optimization of quinazoline-based lead 8 is described. The structure-activity relationship studies indicate the S-configuration is preferred for the phenylmorpholine substitution. Together with incorporation of a (2-hydroxyl-2-methylpropyl)pyrazole moiety at the 2-position leads to analogs...

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Detalhes bibliográficos
Publicado no:Bioorg Med Chem Lett
Main Authors: Yang, Shyh-Ming, Yoshioka, Makoto, Strovel, Jeffrey W., Urban, Daniel J., Hu, Xin, Hall, Matthew D., Jadhav, Ajit, Maloney, David J.
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7405260/
https://ncbi.nlm.nih.gov/pubmed/30905542
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2019.03.014
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