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高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (5): 768-774.doi: 10.1007/s40242-016-6159-6

• Articles • 上一篇    下一篇

Improved Antiproliferative Activities of a New Series of 1,3,4-Thiadiazole Derivatives Against Human Leukemia and Breast Cancer Cell Lines

LIU Tingting, WAN Yichao, LIU Renshuai, MA Lin, LI Minyong, FANG Hao   

  1. Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, P. R. China
  • 收稿日期:2016-04-25 修回日期:2016-06-29 出版日期:2016-10-01 发布日期:2016-07-11
  • 通讯作者: FANG Hao E-mail:haofangcn@sdu.edu.cn
  • 基金资助:

    Supported by the National Natural Science Foundation of China(No.81373281), the Program for New Century Excellent Talents in Universities of China(No.NCET-12-0337) and the Shandong Natural Science Foundation for Distinguished Young Scholars, Chi-na(No.JQ201319).

Improved Antiproliferative Activities of a New Series of 1,3,4-Thiadiazole Derivatives Against Human Leukemia and Breast Cancer Cell Lines

LIU Tingting, WAN Yichao, LIU Renshuai, MA Lin, LI Minyong, FANG Hao   

  1. Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, P. R. China
  • Received:2016-04-25 Revised:2016-06-29 Online:2016-10-01 Published:2016-07-11
  • Contact: FANG Hao E-mail:haofangcn@sdu.edu.cn
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.81373281), the Program for New Century Excellent Talents in Universities of China(No.NCET-12-0337) and the Shandong Natural Science Foundation for Distinguished Young Scholars, Chi-na(No.JQ201319).

摘要：

Twenty-two novel 1,3,4-thiadiazole derivatives were synthesized using different aromatic acids as starting materials, followed by cyclization, coupling and deprotection reaction. The structures of all the target compounds were identified by means of 1H nuclear magnetic resonance(NMR), 13C NMR and high resolution mass spectrometer(HRMS). Further biological evaluations were performed for chronic myelogenous leukemia cell and breast cancer cell. The results suggest that most of the target compounds exhibit potent anti-proliferative activities. Especially, compound 5b shows better antiproliferative activities against MDA-MB-231 and K562 cell lines compared with gossypol.

关键词: Thiadiazole, Anti-tumor activity, Antiproliferative activity

Abstract:

Twenty-two novel 1,3,4-thiadiazole derivatives were synthesized using different aromatic acids as starting materials, followed by cyclization, coupling and deprotection reaction. The structures of all the target compounds were identified by means of 1H nuclear magnetic resonance(NMR), 13C NMR and high resolution mass spectrometer(HRMS). Further biological evaluations were performed for chronic myelogenous leukemia cell and breast cancer cell. The results suggest that most of the target compounds exhibit potent anti-proliferative activities. Especially, compound 5b shows better antiproliferative activities against MDA-MB-231 and K562 cell lines compared with gossypol.

Key words: Thiadiazole, Anti-tumor activity, Antiproliferative activity