Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors.

Clicks: 300
ID: 81109
2020
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Ranked #36 of 246 articles by views in Bioorganic & medicinal chemistry letters

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Abstract
Firstly, a series of Isosteviol derivatives were synthesized and evaluated for FXa inhibitory activity. Among these compounds, the inhibitory activity of compounds 22, 35 and 38 on FXa was better than that of Isosteviol. Secondly, surface plasmon resonance (SPR) assays were performed for selected compounds. Compounds 22, 35, 38 have similar kinetic signatures, and affinity values were at μM level. Thirdly, compounds 22 and 35 displayed moderate-to-high anticoagulation activity and showed similar sensitivity to PT and aPTT. These findings will provide new insight into the exploration of FXa inhibition.
Reference Key
shi2020synthesisbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Shi, Yang;Pan, Bo-Wen;Li, Wen-Chao;Wang, Qing;Wu, Qiong;Pan, Meng;Fu, Hong-Zheng;
Journal Bioorganic & medicinal chemistry letters
Year 2020
DOI
S0960-894X(19)30500-1
URL
Keywords
fxa inhibitors isosteviol structural modification

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