Synthesis, preliminary structure-activity relationships and biological evaluation of pyridinyl-4,5-2H-isoxazole derivatives as potent antitumor agents
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- 作者：Hongliang Yang ; Guoxing Xu ; Yazhong Pei
- 关键词：Pyridine ; Isoxazole ; Anticancer activity ; Chemotherapeutic agent
- 刊名：Chemical Research in Chinese Universities
- 出版年：2017
- 出版时间：February 2017
- 年：2017
- 卷：33
- 期：1
- 页码：61-69
- 全文大小：
- 刊物主题：Chemistry/Food Science, general; Analytical Chemistry; Inorganic Chemistry; Organic Chemistry; Physical Chemistry;
- 出版者：Jilin University and The Editorial Department of Chemical Research in Chinese Universities
- ISSN：2210-3171
- 卷排序：33
文摘
A series of novel pyridinyl-4,5-2H-isoxazole derivatives was synthesized and their chemical structures were characterized by 1H NMR, 13C NMR as well as MS spectroscopic methods, their melting points were also determined. The inhibitory effects of them against breast cancer cell line(MCF-7) were evaluated by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide(MTT) procedure in vitro. Most of them possesed potent anti-proliferative activities, among which 11c and 11j exhibited half maximal inhibitory concentrations(IC50) of 1.9 and 1.5 μmol/L, respectively. These compounds also exhibited potent anti-proliferative activities against both human hepatoma cell line(HepG2) and cervical cancer cell line(Hela). Preliminary Structure-activity relationship(SAR) information from these compounds can be used to guide further exploration of new compounds with better potency as molecular probes. Further study on the mechanism-of-action of these compounds is under investigation.