Synthesis and in vitro antiproliferative activity of new benzothiazole derivatives
Synthesis and in vitro antiproliferative activity of new benzothiazole derivatives
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DOI：
10.3998/ark.5550190.0009.f20
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发表时间：
2008-09
期刊：
影响因子：
0.9
通讯作者：
Yaseen A. Al-Soud;H. Al-Sa’doni;B. Saeed;Ihsan H. Jaber;Mohammad O. Beni-Khalid;N. Al-Masoudi;Tahsin Abdul-Kadir;P. Colla;Bernardetta Busonera;T. Sanna;R. Loddo
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文献类型：
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作者：
Yaseen A. Al-Soud;H. Al-Sa’doni;B. Saeed;Ihsan H. Jaber;Mohammad O. Beni-Khalid;N. Al-Masoudi;Tahsin Abdul-Kadir;P. Colla;Bernardetta Busonera;T. Sanna;R. Loddo
合成了一系列含苯并噻唑的哌嗪-芳基磺酰胺（5a-k）和芳基硫醇类似物（6a-j），以及含磺酰胺（9b、9l-n和10）的取代苯并噻唑。所有化合物在体外对大量人类肿瘤来源细胞系的抗增殖活性进行了评估。化合物5c， 5d, 5j, 6b， 6c和6j是该系列中最有效的类似物，对来自血液病和实体瘤的细胞系都有活性（CC50范围= 8-24µM），只有5d被发现是选择性的，对正常人体组织没有细胞毒性。
A series of benzothiazole bearing piperazino-arylsulfonamides (5a-k), and arylthiol analogues (6a-j) as well as substituted benzothiazoles having sulfonamides (9b, 9l-n and 10) have been synthesized. All compounds were evaluated, in vitro, for their antiproliferative activity against a large panel of human tumor-derived cell lines. Compounds 5c, 5d, 5j, 6b, 6c and 6j were the most potent analogues in this series, showing activity against both cell lines derived from haematological and solid tumors (CC50 range = 8-24 µM), only 5d was found to be selective and not cytotoxic to normal human tissues.