Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (2): 417-424.DOI: 10.6023/cjoc201507038 Previous Articles     Next Articles

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新型1,3,4-噻二唑衍生物的合成及抗肿瘤活性

刘婷婷, 万义超, 方浩   

  1. 山东大学药学院 济南 250012
  • 收稿日期:2015-07-29 修回日期:2015-09-13 发布日期:2015-10-23
  • 通讯作者: 方浩 E-mail:haofangcn@sdu.edu.cn

Synthesis and Antiproliferative Activity of Novel 1,3,4-Thiadiazole Derivatives

Liu Tingting, Wan Yichao, Fang Hao   

  1. Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan 250012
  • Received:2015-07-29 Revised:2015-09-13 Published:2015-10-23

Twenty eight novel 1,3,4-thiadiazole derivatives were synthesized using different phenylacetic acids as the starting material, followed by the reaction of cyclization, coupling, deprotection, and finally introduced different substituted benzenesulfonamides. The structures of all target compounds were identified by 1H NMR, 13C NMR and HRMS. The biological evaluation was performed on PC-3 (prostatic cancer cell), MDA-MB-231 (breast cancer cell) and K562 (chronic myelogenous leukemia cell) by 3-(4,5-dimethylthigal-2-yl)-2,5-(diphenyltetragalium) bromide (MTT) assay. The results suggested that some compounds exhibited good anti-proliferative activities against tumor cell lines. Especially, compounds 6a and 6b showed similar inhibitory activities against K562 cell compared with gossypol.

Key words: thiadiazole, anticancer activity, synthesis