92830-99-4Relevant articles and documents
6-Hydroxy-benzofuran-3-(2H)-ones as Potential Anti-Inflammatory Agents: Synthesis and Inhibitory Activity of LPS-Stimulated ROS Production in RAW 264.7 Macrophage
Shrestha, Aarajana,Shrestha, Ritina,Lee, Sumin,Park, Pil-Hoon,Lee, Eung-Seok
supporting information, p. 372 - 375 (2021/02/11)
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Diversity-oriented synthesis of benzofuro[3,2-b]pyridine derivatives from aurone-derived α,β-unsaturated imines and activated terminal alkynes
Cheng, Bin,He, Yixuan,Li, Hui,Sun, Haiyan,Wang, Taimin,Zhai, Hongbin,Zhang, Xinping,Zhu, Xuecheng
supporting information, p. 7701 - 7704 (2021/08/09)
An efficient annulation reaction of aurone-derived α,β-unsaturated imines and activated terminal alkynes mediated by triethylamine is described, which enables the facile synthesis of 1,4-dihydrobenzofuro[3,2-b]pyridines in high yields. When the nucleophil
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect islet β-cells from apoptosis
Wang, Sheng,Xu, Lei,Lu, Yu-Ting,Liu, Yu-Fei,Han, Bing,Liu, Ting,Tang, Jie,Li, Jia,Wu, Jiangping,Li, Jing-Ya,Yu, Li-Fang,Yang, Fan
, p. 195 - 208 (2017/03/02)
Death-associated protein kinase-related apoptosis-inducing kinase-2 (DRAK2) is a serine/threonine kinase that plays a key role in a wide variety of cell death signaling pathways. Inhibition of DRAK2 was found to efficiently protect islet β-cells from apoptosis and hence DRAK2 inhibitors represent a promising therapeutic strategy for the treatment of diabetes. Only very few chemical entities targeting DRAK2 are currently known. We carried out a high throughput screening and identified compound 4 as a moderate DRAK2 inhibitor with an IC50value of 3.15?μM. Subsequent SAR studies of hit compound 4 led to the development of novel benzofuran-3(2H)-one series of DRAK2 inhibitors with improved potency and favorable selectivity profiles against 26 selected kinases. Importantly, most potent compounds 40 (IC50?=?0.33?μM) and 41 (IC50?=?0.25?μM) were found to protect islet β-cells from apoptosis in dose-dependent manners. These data support the notion that small molecule inhibitors of DRAK2 represents a promising strategy for the treatment of diabetes.