In-vitro anti-HIV and antitumor activity of new 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles and thiadiazine analogues

被引:34
作者
Al-Soud, Yaseen A. [1 ]
Al-Masoudiz, Najim A. [2 ]
Loddo, Robert [3 ]
La Colla, Paola [3 ]
机构
[1] Univ Al Al Bayt, Coll Sci, Dept Chem, Al Mafraq, Jordan
[2] Univ Konstanz, Fachbereich Chem, Constance, Germany
[3] Univ Cagliari, Dept Biomed Sci & Technol, Monserrato, Italy
关键词
anti-HIV activity; antitumor activity; microwave-assisted synthesis; triazolothiadiazoles; thiadiazines;
D O I
10.1002/ardp.200700272
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
A series of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (7-15) and the thiadiazine analogues 16-18 have been synthesized under microwave irradiation (MWI). All synthesized compounds are evaluated for their antiviral activity against the replication of HIV-1 and HIV-2 activity in MT-4. However, compounds 12 and 18 showed EC50 = 2.11 and 1.97 mu g/mL. The results suggest that these compounds can be considered as a new lead in the development of antiviral agents. Compounds 4-18 were tested in vitro against a panel of tumor cell lines. All compounds are inactive against all the tumor sub-lines, except 10 which exhibited activity against CD4(+) human acute T-lymphoblastic leukaemia of CC50 = 64 mu M.
引用
收藏
页码:365 / 369
页数:5
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