1346513-25-4Relevant articles and documents
Synthesis and SAR study of modulators inhibiting tRXRα-dependent AKT activation
Wang, Zhi-Gang,Chen, Liqun,Chen, Jiebo,Zheng, Jian-Feng,Gao, Weiwei,Zeng, Zhiping,Zhou, Hu,Zhang, Xiao-Kun,Huang, Pei-Qiang,Su, Ying
, p. 632 - 648 (2013/05/09)
RXRα represents an intriguing and unique target for pharmacologic interventions. We recently showed that Sulindac and a designed analog could bind to RXRα and modulate its biological activity, including inhibition of the interaction of an N-terminally truncated RXRα (tRXRα) with the p85α regulatory subunit of phosphatidylinositol-3-OH kinase (PI3K). Here we report the synthesis, testing and SAR of a series of novel analogs of Sulindac as potential modulators for inhibiting tRXRα-dependent AKT activation. A new compound 30 was identified to have improved biological activity.