Synthesis and cytotoxic activity of heterocycle-substituted phthalimide derivatives

被引:20
作者
Yang, Ya Jun [1 ,2 ]
Yang, Ya Nan [1 ,2 ]
Jiang, Jian Shuang [1 ,2 ]
Feng, Zi Ming [1 ,2 ]
Liu, Hong Yan [1 ,2 ]
Pan, Xian Dao [1 ,2 ,3 ]
Zhang, Pei Cheng [1 ,2 ]
机构
[1] Peking Union Med Coll, Inst Mat Med, Minist Educ, Key Lab Bioact Subst & Resources Utilizat Chinese, Beijing 100050, Peoples R China
[2] Chinese Acad Med Sci, Beijing 100050, Peoples R China
[3] Beijing Union Pharmaceut Factory, Beijing 102600, Peoples R China
关键词
Phthalimide; Heterocycle; alpha-Bromoketone; Cytotoxic activity; ANTIINFLAMMATORY ACTIVITY; RECEPTOR ANTAGONISTS; THALIDOMIDE; INHIBITORS; DESIGN; ANALOGS;
D O I
10.1016/j.cclet.2010.03.039
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of heterocycle-substituted phthalimide derivatives were synthesized. Structurally diverse derivatives with heterocyclic rings, including furan, imidazo[1,2-a]pyridine, 1,3,4-thiadiazine, imidazo[2,1-b][1,3,4]thiadiazine, pyrazole, 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine, thiazole and thiazoline, were obtained by the reactions of alpha-bromoketone intermediate with various nucleophiles containing oxygen, nitrogen and sulfur atom. Their cytotoxic activity was also evaluated against five human cancer cell lines in vitro. (C) 2010 Pei Cheng Zhang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
引用
收藏
页码:902 / 904
页数:3
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