Synthesis and SAR study of modulators inhibiting tRXRα-dependent AKT activation

ZG Wang, L Chen, J Chen, JF Zheng, W Gao…

Index: Wang, Zhi-Gang; Chen, Liqun; Chen, Jiebo; Zheng, Jian-Feng; Gao, Weiwei; Zeng, Zhiping; Zhou, Hu; Zhang, Xiao-Kun; Huang, Pei-Qiang; Su, Ying European Journal of Medicinal Chemistry, 2013 , vol. 62, p. 632 - 648

Full Text: HTML

Citation Number: 9

Abstract

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 ...