In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

被引:166
作者
Akhtar, Tashfeen [1 ]
Hameed, Shahid [1 ]
Al-Masoudi, Najim A. [2 ]
Loddo, Roberta [3 ]
La Colla, Paolo [3 ]
机构
[1] Quaid I Azam Univ, Dept Chem, Islamabad 45320, Pakistan
[2] Fachbereich Chem Univ, D-78457 Constance, Germany
[3] Univ Cagliari, Dept Biomed Sci & Technol, I-09042 Monserrato, CA, Italy
关键词
1,3,4-oxathiazoles; substituted benzothiazoles; antitumor activity; antiviral activity;
D O I
10.2478/v10007-008-0007-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A series of new benzothiazole derivatives 6a-h have been synthesized, in five steps, from substituted phenols via the 1,3,4-oxadiazole-2-thiones 5a-h. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong effects on leukaemia cell lines CCRF-CEM (CC50 = 12 +/- 2 mu mol L-1, 8 +/- 1 mu mol L-1, respectively). These compounds are leading candidates for further development. The title compounds were tested against representatives of several virus families containing single stranded RNA genomes, either positive-sense (ssRNA+), or negative- sense (RNA-), and against double-stranded RNA genomes (dsRNA), as well as some Flaviviridae viruses.
引用
收藏
页码:135 / 149
页数:15
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