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
相关论文
共 26 条
[21]  
Shafique E, 2015, FASEB J, V29
[22]   Synthesis and Biological Activities of 3-Methoxy-6-substituted-5,6-dihydropyrrolo[3,4-b]pyridin-7-ones [J].
Sun, Guanglong ;
Zhang, Weiwei ;
Zhan, Xiaoping ;
Liu, Zenglu ;
Mao, Zhenmin .
CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2014, 34 (03) :546-551
[23]   Synthesis of Dual Target CPT-Ala-Nor Conjugates and Their Biological Activity Evaluation [J].
Zhao, Chang K. ;
Xu, Lang ;
Wang, Xian H. ;
Bao, Yu J. ;
Wang, Yuhe .
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2019, 19 (04) :502-508
[24]   The regio-selective synthesis of 10-hydroxy camptothecin norcantharidin conjugates and their biological activity evaluation in vitro [J].
Zhao, Chang K. ;
Li, Chan ;
Wang, Xian H. ;
Bao, Yu J. ;
Yang, Fu H. ;
Huang, Mei .
ROYAL SOCIETY OPEN SCIENCE, 2018, 5 (06)
[25]   A simple route to a novel acid-sensitive 20(S)-O-linked camptothecin norcantharidin acid ester derivative [J].
Zhao, Changkuo ;
Wang, Xianheng ;
Yang, Fuhong ;
Gao, Lei ;
Wang, Yuhe .
ROYAL SOCIETY OPEN SCIENCE, 2018, 5 (02)
[26]   Thiothalidomides:: Novel isosteric analogues of thalidomide with enhanced TNF-α inhibitory activity [J].
Zhu, XX ;
Giordano, T ;
Yu, QS ;
Holloway, HW ;
Perry, TA ;
Lahiri, DK ;
Brossi, A ;
Greig, NH .
JOURNAL OF MEDICINAL CHEMISTRY, 2003, 46 (24) :5222-5229