吡喃葡萄糖基共轭苄基衍生物作为新型结肠癌选择性细胞毒剂的合成及药理学特性研究
Synthesis and pharmacological characterization of glucopyranosyl-conjugated benzyl derivatives as novel selective cytotoxic agents against colon cancer.
作者信息
Fu Boqiao, Li Yingjie, Peng Shaoyong, Wang Xiaolin, Hu Jingying, Lv Long, Xia Caifen, Lu Dai, Qin Caiqin
机构信息
Hubei Provincial Collaborative Innovation Center of Biomass Resources Transformation and Utilization, College of Chemistry and Materials Science, Hubei Engineering University, Hubei 432000, People's Republic of China.
Guangdong Institute of Gastroenterology, Guangdong Provincial Key Laboratory of Colorectal and Pelvic Floor Diseases, The Sixth Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong 510655, People's Republic of China.
出版信息
R Soc Open Sci. 2021 Feb 24;8(2):201642. doi: 10.1098/rsos.201642.
Glucopyranosyl-conjugated benzyl derivatives containing a [1,2,3]-triazole linker were synthesized. Benzyl served as an important pharmacophore in anti-cancer compounds. Compound inhibited the proliferation of colorectal cancer cells with the potency comparable to 5-fluorouracil (5-FU) with improved selectivity towards cancer cells. The antiproliferative activity of is achieved through triggering apoptotic cell death.
合成了含有[1,2,3]-三唑连接基的吡喃葡萄糖基共轭苄基衍生物。苄基是抗癌化合物中的重要药效基团。该化合物抑制结肠癌细胞的增殖，其效力与5-氟尿嘧啶（5-FU）相当，且对癌细胞的选择性有所提高。该化合物的抗增殖活性是通过引发凋亡性细胞死亡来实现的。
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