Novel Bis-Artemisinin-Phloroglucinol hybrid molecules with dual anticancer and immunomodulatory Activities: Synthesis and evaluation

被引：1

作者：

Xu, Wei ^{[1
]}

Zou, Xiaosu ^{[2
]}

Zha, Yufeng ^{[3
]}

Zhang, Jinghua ^{[1
]}

Bian, Hongzhu ^{[3
]}

Shen, Zhengwu ^{[1
,2
]}

机构：

[1] Shanghai Jiao Tong Univ, Sch Med, 280 South Chongqing Rd, Shanghai 200025, Peoples R China

[2] Shanghai Univ Tradit Chinese Med, Sch Pharm, 1200 Cai Lun Rd, Shanghai 201203, Peoples R China

[3] Yunnan Baiyao Grp Co Ltd, 3686 Yunnan Baiyao St, Kunming 650200, Peoples R China

来源：

BIOORGANIC CHEMISTRY | 2023年 / 139卷

基金：

中国国家自然科学基金;

关键词：

Artemisinin; Dimer; Anticancer; Immunosuppression; IMMUNOSUPPRESSIVE ACTIVITY; QINGHAOSU ARTEMISININ; ANTIVIRAL ACTIVITIES; IN-VITRO; ANTIMALARIAL; DERIVATIVES; CANCER; DIMERS; CYTOTOXICITY; MECHANISMS;

D O I：

10.1016/j.bioorg.2023.106705

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Bis-(10-deoxydihydroartemisinin)-phloroglucinol (9), has been synthesized in a one-step reaction and has demonstrated strong inhibition to cancer cell proliferation and immunosuppressive activity. The structure modification of the compound reduced its cytotoxicity, and among the analogs, bis-(10-deoxydihydroartemisinin)-phloroglucinol phenyl decanoate (16) showed significant reduction of ear swelling in a mouse model for DNFB-induced delayed-type hypersensitivity without observable toxicity in a dose-dependent manner.

引用

页数：13

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