Design and synthesis of tricyclic sulfones as γ-secretase inhibitors with greatly reduced Notch toxicity
摘要:
A novel series of tricyclic gamma-secretase inhibitors was designed and synthesized via a conformational analysis of literature compounds. The preliminary results have shown that compounds in this new series have much improved in vitro potency and in vivo profiles. More importantly, they have greatly reduced Notch related toxicity that was associated with previous gamma-secretase inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2010.02.080
作为产物:
描述:
C17H17ClF2O4S 在
sodium hydride 作用下,
生成
参考文献:
名称:
Design and synthesis of tricyclic sulfones as γ-secretase inhibitors with greatly reduced Notch toxicity
摘要:
A novel series of tricyclic gamma-secretase inhibitors was designed and synthesized via a conformational analysis of literature compounds. The preliminary results have shown that compounds in this new series have much improved in vitro potency and in vivo profiles. More importantly, they have greatly reduced Notch related toxicity that was associated with previous gamma-secretase inhibitors. (C) 2010 Elsevier Ltd. All rights reserved.