Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers.

Basic Information

ID: ALA3763026

Journal: Bioorg Med Chem Lett

Title: Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers.

Authors: Singh S, Gajulapati V, Gajulapati K, Goo JI, Park YH, Jung HY, Lee SY, Choi JH, Kim YK, Lee K, Heo TH, Choi Y.

Abstract: A series of oxazolidinone and indole derivatives were synthesized and evaluated as IL-6 signaling blockers by measuring the effects of these compounds on IL-6-induced luciferase expression in human hepatocarcinoma HepG2 cells transfected with p-STAT3-Luc. Among different compounds screened, compound 4d was emerged as the most potent IL-6 signaling blockers with IC50 value of 5.9 μM which was much better than (+)-Madindoline A (IC50=21 μM), a known inhibitor of IL-6.

CiteXplore: 26810262

DOI: 10.1016/j.bmcl.2016.01.016

Patent ID: