Design,Synthesis and Antitumor Activity of Fluoroquinolone C3 Heterocyclic Bis-oxadiazole Methylsulf

来源 :Chemical Research in Chinese Universities | 被引量 : 0次 | 上传用户:wb5019
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To discover an efficient route for the shift from an antibacterial fluoroquinolone to an antitumor one based on the mechanistic similarities between targeting topoisomerases and the eukaryotic ones,two series of the title compounds,C3 bis-oxadiazole methylsulfides 6a―6h and corresponding dimethylpiperazinium iodides 7a―7h derived from levofloxacin 1 were designed and synthesized.Their in vitro antiproliferative activities against Chinese hamster ovary cell line(CHO),murine leukemia cell line(L1210) and human leukocytoma cell line(HL60) were evaluated by MTT assay,and inhibitory effect on DNA topoisomerase IIα was also measured by means of densitometric assay. To discover an efficient route for the shift from an antibacterial fluoroquinolone to an antitumor one based on the mechanistic similarities between targeting topoisomerases and the eukaryotic ones, two series of the title compounds, C3 bis-oxadiazole methylsulfides 6a-6h and corresponding dimethylpiperazinium iodides 7a- 7h derived from levofloxacin 1 were designed and synthesized. Their in vitro antiproliferative activities against Chinese hamster ovary cell line (CHO), murine leukemia cell line (L1210) and human leukocytoma cell line (HL60) were evaluated by MTT assay, and inhibitory effect on DNA topoisomerase IIα was also measured by means of densitometric assay.
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