Synthesis and anti-tumor activity of Z-Gly-Pro-OH-podophyllotoxin derivatives
10.11665/j.issn.1000-5048.20220105
- VernacularTitle:N-苄氧羰基甘氨酰-L-脯氨酸-鬼臼毒素衍生物的合成及其抗肿瘤活性
- Author:
Guangping LIANG
1
;
Jun YANG
;
Yunqiu WU
;
Luping WAN
;
Lijun RUAN
;
Zhijun SONG
Author Information
1. 遵义医药高等专科学校药学系
- Publication Type:Journal Article
- Keywords:
podophyllotoxin;
derivative;
synthesis;
anti-tumor;
Z-Gly-Pro-OH
- From:
Journal of China Pharmaceutical University
2022;53(1):32-40
- CountryChina
- Language:Chinese
-
Abstract:
Ten novel podophyllotoxin derivatives (IIIa-IIIi and IV) were synthesized by three-step reactions using podophyllotoxin and N-benzyloxycarbonyl glycine-L-proline as raw material. The structures of the target compounds were confirmed by 1H NMR, 13C NMR and MS. MTT method was used to test anti-tumor activity of the target compounds on HepG2, THP-1, HeLa and MCF-7 cells. The results showed that all the target compounds had inhibitory activity against HepG2, THP-1, HeLa and MCF-7 cells, and the inhibitory activity of IIIa on HepG2 cells was the most prominent with an IC50 value of 0.58 nmol/L. The binding mode of compound IIIa and FAPα was studied by molecular docking. Compound IIIa could bind to multiple sites of FAPα enzyme.
