Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity

[Image: see text] Highly selective PI3K inhibitors with subnanomolar PI3Kα potency and greater than 7000-fold selectivity against mTOR kinase were discovered through structure-based drug design (SBDD). These tetra-substituted thiophenes were also demonstrated to have good in vitro cellular potency a...

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Detalhes bibliográficos
Main Authors: Liu, Kevin K.-C., Zhu, JinJiang, Smith, Graham L., Yin, Min-Jean, Bailey, Simon, Chen, Jeffrey H., Hu, Qiyue, Huang, Qinhua, Li, Chunze, Li, Qing J., Marx, Matthew A., Paderes, Genevieve, Richardson, Paul F., Sach, Neal W., Walls, Marlena, Wells, Peter A., Zou, Aihua
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2011
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4018126/
https://ncbi.nlm.nih.gov/pubmed/24900269
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200126j
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