Synthesis, cytotoxicity, and in vivo antitumor activity study of parthenolide semicarbazones and thiosemicarbazones

被引：24

作者：

Jia, Xinxin ^{[1
]}

Liu, Qi ^{[1
]}

Wang, Shiyi ^{[1
]}

Zeng, Binglin ^{[2
,3
]}

Du, Guohua ^{[2
,3
]}

Zhang, Chen ^{[1
,4
]}

Li, Yan ^{[2
,3
]}

机构：

[1] Beijing Inst Petrochem Technol, Sch Chem Engn, Beijing 102617, Peoples R China

[2] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China

[3] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Act Subst Discovery & Druggabil E, Beijing 100050, Peoples R China

[4] Beijing Inst Petrochem Technol, Beijing Key Lab Enze Biomass Fine Chem, Beijing 102617, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2020年 / 28卷 / 13期

关键词：

FACTOR-KAPPA-B; SESQUITERPENE LACTONES; BIOLOGICAL EVALUATION; CANCER; DESIGN; APOPTOSIS; CELLS; DERIVATIVES; ANTICANCER; INHIBITORS;

D O I：

10.1016/j.bmc.2020.115557

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：

Parthenolide is an important sesquiterpene lactone with potent anticancer activities. In order to further improve its biological activity, a series of parthenolide semicarbazone or thiosemicarbazone derivatives was synthesized and evaluated for their anticancer activity. Derivatives were tested in vitro against 5 human tumor cell lines, and many of these showed higher cytotoxicity than parthenolide. Five compounds were further studied for their antitumor activity in mice. The in vivo result indicated that compound 4d showed both promising antitumor activity against mice colon tumor and small side effects on immune systems. The cell apoptosis and cell cycle distribution of compound 4d were also studied. Molecular docking studies revealed multiple interactions between 4d and NF-κB. Our findings demonstrate the potential of semicarbazones as a promising type of compounds with anticancer activity. © 2020 Elsevier Ltd

引用

页数：10

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