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.
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页数：13
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