Design, Synthesis, and Cytotoxic Evaluation of Novel Lupane Triterpenoid Derived Hydroxamates

被引：5

作者：

Dang Thi Tuyet Anh ^{[1
,2
]}

Dinh Thi Cuc ^{[1
,2
]}

Le Nhat Thuy Giang ^{[1
,2
]}

Nguyen Thi Hien ^{[3
]}

Vu Ngoc Doan ^{[4
]}

Nguyen Ha Thanh ^{[1
]}

Nguyen Van Tuyen ^{[1
,2
]}

Phan Van Kiem ^{[2
,5
]}

机构：

[1] Vietnam Acad Sci & Technol VAST, Inst Chem, Hanoi, Vietnam

[2] Grad Univ Sci & Technol, Hanoi, Vietnam

[3] Vietnam Natl Univ Agr, Fac Environm, Hanoi, Vietnam

[4] Le Quy Don Tech Univ, Hanoi, Vietnam

[5] Vietnam Acad Sci & Technol VAST, Inst Marine Biochem, Hanoi, Vietnam

来源：

NATURAL PRODUCT COMMUNICATIONS | 2020年 / 15卷 / 06期

关键词：

triterpenoid; betulin; betulinic acid; hydroxamate; cytotoxic activity; HISTONE DEACETYLASE INHIBITORS; BETULINIC ACID; EXPRESSION; DERIVATIVES; PROGNOSIS; CANCER;

D O I：

10.1177/1934578X20931967

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5--dimethylthiazol-2--yl]-2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives possess at least moderate cytotoxic activity and the hydroxamate derivative compounds 3c, 3e, 7a, and 15b could be lead compounds for further optimization to develop novel anticancer agents.

引用

页数：8

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