Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities

Wang Jianbin; Wu Menghua; Gao ChunFu Hongzheng

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Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities

机译：Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities

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摘要

Kirenol is one of the biologically active diterpenoids from Siegesbeckia pubescens. In terms of the high content and typical structure, many ent-diterpenoids separated from S. pubescens were presumed to be biologically related to kirenol. Among them, epoxy-pimarane diterpenoids are belonging to a special family of naturally occurring compounds that attracted our attentions on their putative biosynthesis pathway and biological activities. Here, we designed and synthesized two known 14,16-epoxy-pimarane diterpenoids (2 and 3) and five 8,15-epoxypimarane diterpenoids (4-8) from kirenol. Their absolute structures were determined by 1D and 2D NMR data and the absolute configurations of 4 were confirmed by X-ray crystallographic data. Their inhibition effects on factor Xa (FXa) were evaluated to assess the potentiality of epoxy-pimarane diterpenoids as FXa inhibitor agents.

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来源
《Bioorganic and medicinal chemistry》 |2019年第7期|1320-1326|共7页
作者
Wang Jianbin; Wu Menghua; Gao ChunFu Hongzheng;
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作者单位

Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China;

Jian Univ, Coll Pharm, Res Ctr Tradit Chinese Med Lingnan Southern China, Guangzhou 510632;

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正文语种英语
中图分类药学;
关键词
Kirenol; Siegesbeckia; Siegesbeckia pubescens; Epoxy-pimarane diterpenoids; X-ray crystallographic data; Factor Xa;

Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities

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