Singh Sarbjit, Gajulapati Veeraswamy, Gajulapati Kondaji, Goo Ja-Il, Park Yeon-Hwa, Jung Hwa Young, Lee Sung Yoon, Choi Jung Ho, Kim Young Kook, Lee Kyeong, Heo Tae-Hwe, Choi Yongseok
College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea; College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
Bioorg Med Chem Lett. 2016 Feb 15;26(4):1282-6. doi: 10.1016/j.bmcl.2016.01.016. Epub 2016 Jan 9.
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.
合成了一系列恶唑烷酮和吲哚衍生物，并通过测量这些化合物对转染了p-STAT3-Luc的人肝癌HepG2细胞中IL-6诱导的荧光素酶表达的影响，来评估它们作为IL-6信号传导阻滞剂的活性。在筛选的不同化合物中，化合物4d表现为最有效的IL-6信号传导阻滞剂，IC50值为5.9 μM，远优于已知的IL-6抑制剂(+)-马吲哚啉A（IC50 = 21 μM）。
