Synthesis and biological evaluation of camptothecin substituted norcantharimide derivatives

被引:5
作者
Lan, Qing [1 ]
Zhou, Yiqi [1 ]
Wang, Xianheng [1 ]
Wang, Yuhe [2 ]
Zhao, Changkuo [1 ]
机构
[1] Zunyi Med Univ, Dept Med Chem, Zunyi, Guizhou, Peoples R China
[2] Zunyi Med Univ, Affiliated Hosp, Dept Pharm, Zunyi, Guizhou, Peoples R China
关键词
Thalidomide; cantharidimide; cnticancer; camptothecin; THALIDOMIDE; METABOLITES;
D O I
10.1080/14786419.2020.1834546
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
In this paper, a series of novel derivatives of camptothecin substituted norcantharimide was designed by mimic strategy. These compounds were synthesized in moderate yields by directly coupling CPT with N-amino acid norcantharimides. Their cytotoxicity to four human tumour cell lines (HepG2, BGC-803, SW480 and PANC-1) and normal human cell lines L-O2 and HIEC was evaluated. The synthesized CPT substituted norcantharimide analogs (3g and 3f) showed better anti-hepatocarcinoma activity than CPT. Compounds 3d, 3e, 3g, 3h and 3i also showed strong inhibition activity against BGC803. [GRAPHICS] .
引用
收藏
页码:5752 / 5756
页数:5
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