Synthesis and anti-tumor activity of Z-Gly-Pro-OH-podophyllotoxin derivatives / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 32-40, 2022.
Article
in Chinese
| WPRIM
| ID: wpr-920647
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.
Full text:
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Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Journal of China Pharmaceutical University
Year:
2022
Type:
Article
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