Acta Chimica Sinica ›› 2011, Vol. 69 ›› Issue (21): 2561-2566.DOI: 10.6023/A1103214B Previous Articles     Next Articles

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  1. (天津理工大学化学化工学院 天津 300384)
  • 投稿日期:2011-03-21 修回日期:2011-06-19 发布日期:2011-07-12
  • 通讯作者: 陈宝泉
  • 基金资助:


Synthesis and Antitumor Activity of 2-(2-Substituted 1,3,4-thiadiazol-5-yl)benzisoselenazol-3(2H)-one Derivatives

SHI Yan-Ping, CHEN Bao-Quan, MA Jing, LIU Yu-Ming, LI Cai-Wen   

  1. (School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384)
  • Received:2011-03-21 Revised:2011-06-19 Published:2011-07-12

Ten novel 2-(2-substituted 1,3,4-thiadiazol-5-yl)benzisoselenazol-3(2H)-one derivatives (6) were synthesized by the condensation of 2-chloroselenobenzoyl chloride and 2-amino-5-substituted 1,3,4-thiadiazole according to substructure link principle, and structurally confirmed by IR, 1H NMR, ESI-MS techniques and elemental analysis. The antiproliferative activities against three tumor cells were tested using CCK-8 method. The results indicated that 6h against A-549, 6a, 6b, 6d, 6e, 6f, 6g, 6h, 6j against MCF-7 and 6a, 6b, 6d, 6e, 6f, 6g against SSMC-7721 showed better activities than positive control Ebselen did, which suggested such compounds with a certain selectivity to the three tumor cells and were worth further investigation.

Key words: selenium, benzisoselenazolone, 1,3,4-thiadiazole, synthesis, antitumor activity