新型4-苯胺喹唑啉β-D-木糖苷的细胞毒性和糖胺聚糖引发活性
Cytotoxic and glycosaminoglycan priming activities of novel 4-anilinequinazoline β-D-xylosides.
作者信息
Wang Jinpeng, Chang Yajing, Dong Xueyang, Zhang Renshuai, Tang Yang, Zhang Meng, Yu Rilei, Jiang Tao, Zhang Lijuan
机构信息
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao, 266003, PR China.
Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 5 Yushan Road, Qingdao, 266003, PR China; Systems Biology & Medicine Center for Complex Diseases, Qingdao, 266071, PR China.
出版信息
Carbohydr Res. 2018 Jun 30;463:6-13. doi: 10.1016/j.carres.2018.04.007. Epub 2018 Apr 13.
β-D-xylosides with cytotoxic aglycones have augmented cytotoxicity towards animal cells because β-D-xyloside-primed glycosaminoglycans further enhance the aglycone's cytotoxicity. In this study, we designed and synthesized different 4-anilinequinazoline β-D-xylosides and found that compounds 7-10 possessing 3-chloro-4-((3-fluorobenzyl)oxy)aniline group as in anticancer drug lapatinib also primed glycosaminoglycans and were highly cytotoxic to cancer cells.
带有细胞毒性苷元的β-D-木糖苷对动物细胞具有增强的细胞毒性，因为经β-D-木糖苷预处理的糖胺聚糖会进一步增强苷元的细胞毒性。在本研究中，我们设计并合成了不同的4-苯胺基喹唑啉β-D-木糖苷，发现具有与抗癌药物拉帕替尼中相同的3-氯-4-((3-氟苄基)氧基)苯胺基团的化合物7-10也能预处理糖胺聚糖，并且对癌细胞具有高度细胞毒性。
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