Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal …

…, J Kaplan, L Toral-Barza, I Hollander, J Lucas…

文献索引：Richard, David J.; Verheijen, Jeroen C.; Curran, Kevin; Kaplan, Joshua; Toral-Barza, Lourdes; Hollander, Irwin; Lucas, Judy; Yu, Ker; Zask, Arie Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 24 p. 6830 - 6835

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被引用次数: 40

摘要

A series of highly potent and selective pyrazolopyrimidine mTOR inhibitors which contain water-solubilizing groups attached to the 6-arylureidophenyl moiety have been prepared. Such derivatives displayed superior potency to those in which these appendages were attached to alternative sites. In comparison to unfunctionalized arylureido compounds, these analogs demonstrated enhanced cellular potency and significantly improved stability ...