3241-77-8Relevant academic research and scientific papers
Synthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists
Wang, Yan-Xiang,Wang, Li,Xu, Yan-Ni,Li, Ying-Hong,Jiang, Jian-Dong,Si, Shu-Yi,Li, Yang-Biao,Ren, Gang,Shan, Yong-Qiang,Hong, Bin,Song, Dan-Qing
experimental part, p. 1066 - 1073 (2011/04/23)
By using human scavenger receptor CD36 as the target, twenty-five N-(2-arylethyl) isoquinoline derivatives were designed, synthesized and evaluated for their antagonistic activities for CD36-oxidatively low density lipoprotein (oxLDL) binding. The primary analysis of structure-activity relationship (SAR) indicated a methoxyl at the 7-position and a hydroxyl at the 6- or 8-position could afford good activities. Among these analogs, compounds 7e and 7t showed the potential CD36 antagonistic activities with IC50 values of 0.2 and 0.8 μg/mL, respectively. Furthermore, both of them could effectively inhibit oxLDL uptake in insect Sf9 cells overexpressing human CD36, and thus have been selected for further investigation. We consider N-(2-arylethyl) isoquinoline analogs to be a family of novel CD36 antagonists.
