2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists

S Kher, K Lake, I Sircar, M Pannala, F Bakir…

Index: Kher, Sunil; Lake, Kirk; Sircar, Ila; Pannala, Madhavi; Bakir, Farid; Zapf, James; Xu, Kui; Zhang, Shao-Hui; Liu, Juping; Morera, Lisa; Sakurai, Naoki; Jack, Rick; Cheng, Jie-Fei Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 16 p. 4442 - 4446

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Citation Number: 15

Abstract

Structure–activity relationship studies on a series of Boc-indole derivatives as LXR agonists are described. Compound 1 was identified as an LXR agonist through structure-based virtual screening followed by high-throughput gene profiling. Replacement of the indan linker portion in 1 with an open-chain linker resulted in compounds with similar or improved in vitro potency and cellular functional activity. The Boc group at the N-1 position of the ...