Synthesis and biological evaluation of camptothecin substituted norcantharimide derivatives

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.

Keywords:

• Thalidomide
• cantharidimide
• cnticancer
• camptothecin

Acknowledgments

I am very grateful for the financial support from Key Project of Guizhou Provincial Administration of Traditional Chinese Medicine (QZYYZD-2019-05), Joint fund project of Science and Technology Foundation of Zunyi City (ZunyiKeHe HZ [2019]26), Guizhou Provincial Administration of Traditional Chinese Medicine (QZYY2017-030), Science and Technology Foundation of Guizhou Province (QianKeHe Platform/talent[2019]5657), Public Bidding Project Foundation of Zunyi Medical University ([2013]F-680), Doctoral Scientific Research Foundation of Zunyi Medical University ([2013]F-633) and [2014]F-697), Science and Technology Foundation of Guizhou Province (QianKeHe ZhiCheng [2019]2829), and I am also very thankful for Dr. Yuqi He’s useful explanation on MS spectrum data.

Disclosure statement

No potential conflict of interest was reported by the author(s).