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2-烷基、2-芳基和2-哌嗪基苯并咪唑-4,7-二酮衍生物的合成及其体外抗肿瘤活性

Synthesis and in vitro antitumor activity of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives.

作者信息

Ahn C M, Tak J A, Choi S J

机构信息

Department of Basic Sciences, Institute of Basic Medical Science, Wonju College of Medicine, Yonsei University, Korea.

出版信息

Arch Pharm Res. 2000 Aug;23(4):288-301. doi: 10.1007/BF02975437.

DOI:10.1007/BF02975437
PMID:10976573
Abstract

A series of 2-alkyl, 2-aryl, and 2-piperazinyl benzimidazole-4,7-dione derivatives (7a-h) and 16m-o) were prepared, and their cytotoxicities were tested against three cancer cell lines (mouse lymphocytic leukemia cell line P388, and human gastric carcinoma cell lines SNU-1 and SNU-16). These compounds showed potent cytotoxicity against all of three cell lines tested, and especially SNU-16 was sensitive to them. 2-Aryl (7g,h) and 2-piperazinyl benzimidazole-4,7-dione derivative (16 m) were more potent than mitomycin C against P388 and SNU-16. Among benzimidazole-4,7-dione derivatives with alkyl group at position 2, 7a had the most potent cytotoxicity against all of the cell lines tested.

摘要

制备了一系列2-烷基、2-芳基和2-哌嗪基苯并咪唑-4,7-二酮衍生物(7a-h)和16m-o),并测试了它们对三种癌细胞系(小鼠淋巴细胞白血病细胞系P388以及人胃癌细胞系SNU-1和SNU-16)的细胞毒性。这些化合物对所有测试的三种细胞系均显示出强效细胞毒性,尤其是SNU-16对它们敏感。2-芳基(7g,h)和2-哌嗪基苯并咪唑-4,7-二酮衍生物(16m)对P388和SNU-16的活性比丝裂霉素C更强。在2位带有烷基的苯并咪唑-4,7-二酮衍生物中,7a对所有测试细胞系的细胞毒性最强。

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