期刊
TURKISH JOURNAL OF BIOCHEMISTRY-TURK BIYOKIMYA DERGISI
卷 42, 期 5, 页码 535-544出版社
WALTER DE GRUYTER GMBH
DOI: 10.1515/tjb-2017-0015
关键词
Benzothiazole; Synthesis; Lung cancer; Cytotoxicity; Apoptosis
Objective(s): In this study, it was aimed to synthesize new chemotherapeutic agents based on known antiproliferative properties of benzothiazol-2-amine moiety. The antitumor activity of the newly synthesized compounds was determined against A549 lung cancer cell lines. Methods: Eighteen compounds were obtained by two steps synthetic route. The anticancer potency of the compounds were detected using MTT assay and flow cytometric analysis on A549 cell line. Some physicochemical properties of the compounds were calculated, virtually. Results: Compounds 15 and 18 showed the highest cytotoxic activity even than cisplatin. Also, it was determined that compound 18 caused 19.1% (early and late) apoptosis whereas cisplatin caused 21.6% (early and late). Conclusion: Considering the calculated virtual data, eighteen new compounds were found within the boundaries of Lipinski rule of five to be an oral drug. Besides, the most potent compounds 15 and 18 were detected that both have 1-methylbenzimidazole structure, and also methoxy and ethoxy substituents on benzothiazole ring.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据