CRCU

Chemical Research in Chinese Universities ›› 2011, Vol. 27 ›› Issue (5): 787-791.

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Design and Synthesis of 3-Substituedmethylenethiochroman-4-ones as Anticancer Agents

MA Zheng-yue, ZHANG Xing-hua, LI Chun-na, ZHENG Ya-jun, YANG Geng-liang*, WANG Shi-kui and HE Yang   

  1. Key Laboratory for Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding 071002, P. R. China
  • Received:2010-10-28 Revised:2011-05-06 Online:2011-09-25 Published:2011-09-06
  • Contact: YANG Geng-liang E-mail:ygl@hbu.edu.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.21175031), the Program for Science and Technology Development of Hebei Province, China(No.11966411D), the Fund of Key Laboratory for Pharmaceutical Quality Control of Hebei Province, China(No.09265631D-14), the Fund of Hebei University, China(No. 2010Q33) and the Fund of Hebei Provincial Department of Education, China(Nos.ZD2010234, 2011159).

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Abstract: A series of 3-substituedmethylenethiochroman-4-ones was designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR, MS, IR, UV and elemental analysis. The results of their anticancer activity studies show that almost all 3-chloromethylenethiochroman-4-ones exhibit high anticancer activities and their activities are all better than reference cisplatin. Their IC50 against cancer cells is in a range of 0.80―9.17 μg/mL. Thus they could be promising candidates for anticancer drugs. However, compound 5 has no activity against cancer cells, thus chloromethylene at the 3 position of thiochroman-4-ones seems to play an important role in observed anticancer activities.

Key words: Anticancer activity, 3-Chloromethylene, Thiochromanone