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OALib Journal期刊
ISSN: 2333-9721
费用：99美元
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氟喹诺酮c-3均三唑硫醚酮及其衍生物的合成和抗肿瘤活性
, PP. 1258-1262
Keywords: 氟喹诺酮,环丙沙星,均三唑,硫醚酮,缩氨基硫脲,噻唑并三唑,抗肿瘤活性
Abstract:
为发现氟喹诺酮由抗菌活性到抗肿瘤活性转化的有效结构修饰策略,以均三唑硫醇(酮)杂环为c-3羧基的等排体,经硫醚化修饰得c-3均三唑硫醚酮(6a～6g),进一步优化得c-3均三唑硫醚酮缩氨基硫脲(7a～7g)和c-3噻唑并三唑稠杂环类(8a～8g)。用元素分析和光谱数据确证化合物的结构,用mtt方法评价3类化合物对hep-3b、capan-1和hl60的体外抗增值活性。结果表明,上述3类化合物的体外抗肿瘤活性均强于环丙沙星,其中相应化合物的活性次序为7>8>6,对肿瘤细胞的选择性为capan-1>hep-3b>hl60。同时,含吸电子基(f、no2)取代的目标化合物(6f、7f、8f和6g、7g、8g)均强于其他取代基目标物的活性,尤其是缩氨基硫脲类(7f、7g)对capan-1的ic50值与对照药多柔比星相当。为此,硫醚酮缩氨基硫脲修饰的均三唑杂环作为c-3羧基等排体值得关注和进一步发展。
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