1. Synthesis and biological evaluation of camptothecin substituted norcantharimide derivatives
- Author
-
Changkuo Zhao, Zhou Yiqi, Qing Lan, Yuhe Wang, and Xianheng Wang
- Subjects
endocrine system diseases ,Stereochemistry ,Antineoplastic Agents ,Plant Science ,01 natural sciences ,Biochemistry ,Analytical Chemistry ,Structure-Activity Relationship ,Cell Line, Tumor ,medicine ,Humans ,heterocyclic compounds ,Cytotoxicity ,neoplasms ,Biological evaluation ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,Human cell ,digestive system diseases ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Cell culture ,Camptothecin ,medicine.drug - Abstract
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.
- Published
- 2020