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

作　　者：LIU Tingting WAN Yichao LIU Renshuai MA Lin LI Minyong FANG Hao 

机构地区：[1]Key Laboratory of Chemical Biology, Ministry of Education, Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Jinan 250012, P. R. China

出　　处：《Chemical Research in Chinese Universities》2016年第5期768-774,共7页高等学校化学研究（英文版）

基　　金：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, China（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 IH nuclear magnetic resonance（NMR）, laC 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.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 IH nuclear magnetic resonance（NMR）, laC 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 

分 类 号：O[理学]