Design, synthesis and biological evaluation of novel hydroxamic acids bearing artemisinin skeleton

被引：21

作者：

Vu Thi Ha ^{[1
]}

Vu Tuan Kien ^{[1
]}

Le Huy Binh ^{[1
]}

Vu Dinh Tien ^{[1
]}

Nguyen Thi Thuy My ^{[1
]}

Nguyen Hai Nam ^{[2
]}

Baltas, Michael ^{[3
]}

Hahn, Hyunggu ^{[4
]}

Han, Byung Woo ^{[4
]}

Do Thi Thao ^{[5
]}

Tran Khac Vu ^{[1
]}

机构：

[1] Hanoi Univ Sci & Technol, Sch Chem Engn, 1 Dai Co Viet, Hanoi, Vietnam

[2] Hanoi Univ Pharm, 13-15 Le Thanh Tong, Hanoi, Vietnam

[3] Univ Toulouse 3, UMR 5068, Synth & Physicochim Mol Interet Biol, 118 Route Narbonne, F-31062 Toulouse 9, France

[4] Seoul Natl Univ, Coll Pharm, Pharmaceut Sci Res Inst, Seoul 151742, South Korea

[5] Vietnam Acad Sci & Technol, Inst Biotechnol, 18 Hoang Quoc Viet, Hanoi, Vietnam

来源：

BIOORGANIC CHEMISTRY | 2016年 / 66卷

基金：

新加坡国家研究基金会;

关键词：

Artemisinin; Histone deacetylase (HDAC) inhibitors; Hydroxamic acids; Endoperoxide; Cytotoxicity; HISTONE-DEACETYLASE INHIBITORS; HDAC INHIBITORS; DERIVATIVES; CANCER; UPDATE;

D O I：

10.1016/j.bioorg.2016.03.008

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：

A series of novel hydroxamic acids bearing artemisinin skeleton was designed and synthesized. Some compounds in this series exhibited moderate inhibition against the whole cell HDAC enzymes. Especially, compound 6g displayed potent cytotoxicity against three human cancer cell lines, including HepG2 (liver cancer), MCF-7 ( breast cancer) and HL-60 (leukemia cancer), with IC50 values of 2.50, 2.62 and 1.28 mu g/mL, respectively. Docking studies performed with two potent compounds 6a and 6g using Autodock Vina showed that both compounds bound to HDAC2 with relatively high binding affinities from -7.1 to 7.0 kcal/mol compared to SAHA (-7.4 kcal/mol). It was found in this research that most of the target compounds seemed to be more cytotoxic toward blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. (C) 2016 Elsevier Inc. All rights reserved.

引用

页码：63 / 71

页数：9

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