108838-36-4Relevant articles and documents
Discovery of 4,6-bis(benzyloxy)-3-phenylbenzofuran as a novel Pin1 inhibitor to suppress hepatocellular carcinoma via upregulating microRNA biogenesis
Fan, Xin,He, Huaiyu,Li, Jiao,Luo, Guoyong,Zheng, Yuanyuan,Zhou, Jian-Kang,He, Juan,Pu, Wenchen,Zhao, Yun
, p. 2235 - 2244 (2019/04/30)
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1)participates in diverse cancer-associated signaling pathways, playing an oncogenic role in multiple human cancers, including hepatocellular carcinoma (HCC). Our recent works clarify that Pin1 modulates miRNAs biogenesis by interacting with ERK-phosphorylated exportin-5 (XPO5)and changing XPO5 conformation, giving a potential target for HCC treatment. Herein, we discover 4,6-bis(benzyloxy)-3-phenylbenzofuran (TAB29)as a novel Pin1 inhibitor that targets Pin1 PPIase domain. TAB29 potently inhibits Pin1 activity with the IC50 value of 874 nM and displays an excellent selectivity toward Pin1 in vitro. Cell-based biological evaluation reveals that TAB29 significantly suppresses cell proliferation of HCC cells through restoring the nucleus-to-cytoplasm export of XPO5 and upregulating mature miRNAs expression. Collectively, this work provides a promising small molecule lead compound for Pin1 inhibition, highlighting the therapeutic potential of miRNA-based treatment for human cancers.
Cationic palladium(II)-catalyzed addition of arylboronic acids to nitriles. One-step synthesis of benzofurans from phenoxyacetonitriles
Zhao, Baowei,Lu, Xiyan
, p. 5987 - 5990 (2007/10/03)
(Chemical Equation Presented) A cationic palladium complex catalyzed addition of arylboronic acids to nitrites to yield aryl ketones with moderate to good yields was developed. A one-step synthesis of benzofurans from phenoxyacetonitriles under the catalysis of [(bpy)Pd+(μ-OH)] 2(-OTf)2 or [(bpy)Pd2+(H 2O2)2](-OTf)2 was developed which showed that the cationic palladium catalyst is highly active for these addition reactions.
Preparation of activated benzofurans and their reactions with aldehydes
Black, David St.C.,Craig, Donald C.,Kumar, Naresh,Rezaie, Robert
, p. 4803 - 4814 (2007/10/03)
Reactions of 3-substituted 4,6-dimethoxybenzofurans with formaldehyde and aryl aldeydes in the presence of acetic acid and phosphoryl chloride respectively give new macrocyclic calix[3]benzofurans, predominantly with an unsymmetrical linkage pattern. Inco