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OALib Journal期刊
ISSN: 2333-9721
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氟喹诺酮(绕丹宁不饱和酮)酰胺衍生物的合成与抗肿瘤活性
, PP. 1008-1012
Keywords: 氟喹诺酮c-3酰胺,绕丹宁,不饱和酮,抗细胞增殖活性
Abstract:
为发现新型抗肿瘤绕丹宁不饱和酮衍生物,以氟喹诺酮酰胺骨架作为载体,设计合成了氟喹诺酮(绕丹宁α,β-不饱和酮)酰胺类目标化合物5a~5r,其结构经元素分析、1hnmr、ms确证。采用mtt法评价了目标化合物对人肝癌hep-3b细胞、人capan-1胰腺癌细胞及人hl60白血病细胞的体外增值抑制活性。结果表明,18个目标化合物对3种实验癌细胞的抗增殖活性均显著高于母体环丙沙星1的活性,其中对capan-1细胞的活性最强,尤其是芳杂环或苯环带有吸电子羧基及磺酰氨基类化合物的活性与对照抗肿瘤药物阿霉素相当。为此,氟喹诺酮(绕丹宁不饱和酮)酰胺衍生物是一类有发展前景的抗肿瘤活性先导物。
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