Biological evaluation of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imine derivatives

被引：56

作者：

Huang, Chao ^{[1
]}

Yan, Sheng-Jiao ^{[1
]}

Zeng, Xiang-Hui ^{[1
]}

Dai, Xiao-Yang ^{[2
]}

Zhang, Yin ^{[2
]}

Qing, Chen ^{[2
]}

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] Kunming Med Univ, Yunnan Key Lab Pharmacol Nat Prod, Kunming 650031, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 04期

基金：

中国国家自然科学基金;

关键词：

Isoquinolin-1(2H)-imine; Polyhalo heterocyclic ketene aminals; Anti-tumour; Acute toxicity; AGENTS; ANTICANCER; ROUTE;

D O I：

10.1016/j.ejmech.2011.01.036

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of polyhalo 1,3-diazaheterocycle fused isoquinolin-1(2H)-imines were evaluated in vitro against human tumour cell lines including A431, K562, HL60, HepG2 and Skov-3. As a result, some of the target compounds such as 5b, 5c, 5i, 5o, 6c, 6h and 7f showed stronger cytotoxicity against K562, H562 and Skov-3 cells in comparison with cisplatin, and the others displayed moderate cytotoxicity to A431 and HepG2. Biological investigations using the representative compounds 5c, 6c and 6h were also performed in mice bearing S(180) and H(22) tumours. The results indicated that these three compounds inhibit S(180) and H22 growth. In addition, compounds 6c and 6h have very low acute toxicities. The preliminary analysis of structure-activity relationships is also discussed. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：1172 / 1180

页数：9

共 23 条

[1] Synthesis of novel steroidal heterocyclic derivatives as antibacterial agents [J].