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OALib Journal期刊
ISSN: 2333-9721
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c-3噁二唑硫乙酰腙取代的氟喹诺酮类似物的合成、抗肿瘤活性及构-效关系
, PP. 1694-1698
Keywords: 氟喹诺酮,噁二唑,酰腙,抗肿瘤活性,构-效关系
Abstract:
为寻找氟喹诺酮由抗菌活性转化为抗肿瘤活性的有效策略,基于药效团拼合原理,用噁二唑替代培氟沙星c-3位羧基,功能酰腙基为其修饰基团,设计合成了c-3噁二唑硫乙酰腙目标化合物7a～7o,目标化合物结构经元素分析、1hnmr、ms确证.采用mtt法评价了目标化合物对人肝癌hep-3b细胞株的体外增殖抑制活性.结果表明,15个目标化合物活性均显著高于对照培氟沙星的活性,其中带吸电子取代基化合物的活性高于供电子基团化合物的活性,尤其是含羧基取代基化合物的活性与对照抗肿瘤药物阿霉素相当,表明芳环羧基修饰基的存在有利于提高抗肿瘤活性.
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