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Volume 49 Number 3


Research articles

ScienceAsia 49 (2023): 38-42 |doi: 10.2306/scienceasia1513-1874.2023.117


Imide cantharidin derivatives: Synthesis and HBV-DNA inhibitory properties


Chun Bin Tana,*, Ya Jing Xinga, Xing Fang Qiaoa,*, Bao Min Fana,b, Xiao-Ling Liua, Yao Bo Zenga,*

 
ABSTRACT:     Cantharidin and its analogs are potent serine/threonine protein phosphatase inhibitors with rare reports on inhibiting expression of Hepatitis B virus (HBV) DNA. Five imide cantharidin derivatives were synthesized, and their properties were studied. The inhibition efficiency was determined, and preliminary studies on the structure-activity relationships were conducted. The results indicated that the compounds characterized by low Log P values and the cantharidin moieties containing nitrogen exhibited low cytotoxicity and helped inhibit the expression of HBV DNA. Compound 2 and the non-cytotoxic compound 3 significantly inhibited the expression of HBV DNA. The IC50 values recorded for both compounds were 2.0?1.2 and 19.2?2.0 nM, respectively.

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a Chongqing Academy of Chinese Materia Mediea, Chongqing 400065 China
b School of Chemistry and Environment, Yunnan Minzu University, Kunming 650503 China

* Corresponding author, E-mail: tcb204@163.com, cqszyy2022@163.com, c0230231111@163.com

Received 11 Feb 2022, Accepted 10 Jun 2022