Synthesis and evaluation of the antitumor activity of polyhalo acridone derivatives

被引：10

作者：

Huang, Chao ^{[1
,2
,3
]}

Yan, Sheng-Jiao ^{[1
]}

Zeng, Xiang-Hui ^{[1
]}

Sun, Bo ^{[4
,5
]}

Lan, Min-Bo ^{[4
,5
]}

Lin, Jun ^{[1
]}

机构：

[1] Yunnan Univ, Sch Chem Sci & Technol, Minist Educ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China

[2] Yunnan Minzu Univ, Sch Chem & Biotechnol, State Ethn Affairs Commiss, Key Lab Ethn Med Resource Chem, Kunming 650050, Peoples R China

[3] Yunnan Minzu Univ, Sch Chem & Biotechnol, Minist Educ, Kunming 650050, Peoples R China

[4] E China Univ Sci & Technol, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China

[5] E China Univ Sci & Technol, Res Ctr Anal & Test, Shanghai 200237, Peoples R China

来源：

RSC ADVANCES | 2015年 / 5卷 / 23期

基金：

芬兰科学院; 中国国家自然科学基金;

关键词：

FLUORESCENT; IDENTIFICATION; DESIGN; CHEMOSENSORS; INHIBITION; PROBE; DNA;

D O I：

10.1039/c4ra12354a

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of polyhalo acridone heterocyclic compounds were synthesized and evaluated for their in vitro antitumor activity. It was noteworthy that halogen atoms were present at the 1, 3 and 4 sites of the compounds, and an amide group or a cyano group was at the 2 site. The antitumor bioactivity screening revealed that all the compounds exhibited potent antitumor activity. In particular, compounds 4d, 4o, 5j and 5k showed good antineoplastic selectivity, with a survival rate above 50% in NIH3T3 mouse embryonic cells. The IC50 values were 8.69-13.06 mu M in A431 cells. A preliminary assessment of the structure-selectivity relationship of the compounds was also performed.

引用

页码：17444 / 17450

页数：7

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