Design, synthesis and antitumor activity of 3-arenobufagin esters
10.12206/j.issn.1006-0111.202007022
- VernacularTitle:沙蟾毒精酯类衍生物的合成和抗肿瘤活性研究
- Author:
Chuan LUO
1
;
Jianjiang MA
2
;
Zhenyuan MIAO
3
;
Yuelin WU
2
Author Information
1. Anhui Huarun Golden Frog Pharmaceutical Co., Ltd., Huaibei 235000, China.
2. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, China.
3. School of Pharmacy, Naval Medical University, Shanghai 200433, China.
- Keywords:
arenobufagin;
drug design;
ester derivatives;
antitumor activity
- From:
Journal of Pharmaceutical Practice
2021;39(1):35-37
- CountryChina
- Language:Chinese
-
Abstract:
Objective To search for novel potent 3-ester derivatives of arenobufagin and test their antitumor activities in vitro. Methods Target compounds were synthesized by esterification of arenobufagin with acids. CellTiter method was used to assay the in vitro antitumor activities. Results 3-Ester derivatives exhibited excellent antitumor activities against all the cancer cells. Conclusion Among the 3-ester derivatives, compound 2a had the best activities with the IC50 of 4.0−91.7 nmol/L and appeared to be a valuable candidate for further study.
