郑州大学学报（医学版）2017，Vol.52Issue(1)：28-33,6.DOI:10.13705/j.issn.1671-6825.2017.01.008
氟喹诺酮 C-3噁二唑硫乙酰腙的合成及抗肿瘤活性测定
Synthesis and antitumor activity detection of fluoroquinolone C-3 oxadi-azole sulfanylacetylhydrazones
摘要
Abstract
Aim:To discover an efficient strategy for a conversion of antibacterial fluoroquinolones into antitumor fluo -roquinolones .Methods:Ten novel fluoroquinolone C-3 oxadiazole sulfanylacetylhydrazone derivatives were designed and synthesized with an oxadiazole ring as the C-3 bioisostere modified by a functionalized sulfanylacetylhydrazone side-chain from ciprofloxacin, respectively.The structures of the title compounds were characterized by elemental analysis and spectral data , and the in vitro antitumor activity against SMMC-7721 , L1210 and HL60 cell lines was evaluated by MTT assay .Re-sults:The title compounds demonstrated more antiproliferative activity than the parent .In particular , compounds bearing a fluorine atom or nitro group attached to benzene ring were comparable to the control doxorubicin .Conclusion: An azole modified with functionalized side-chain as the bioisosteric replacement of the C-3 carboxylic group is favorable to improve-ment of antitumor activity .关键词
氟喹诺酮/噁二唑/酰腙/生物电子等排体/抗肿瘤活性Key words
fluoroquinolone/oxadiazole/acylhydrazone/bioisostere/antitumor activity分类
医药卫生引用本文复制引用
李珂,张会丽,闻婧,胡国强,黄文龙..氟喹诺酮 C-3噁二唑硫乙酰腙的合成及抗肿瘤活性测定[J].郑州大学学报（医学版）,2017,52(1):28-33,6.基金项目
国家自然科学基金面上资助项目20872028，21072045 （）
