Synthesis and antitumor activity of phosphonate derivatives containing amino acid
10.16438/j.0513-4870.2016-0041
- VernacularTitle:含氨基酸片段的膦酸酯衍生物合成与抗肿瘤作用
- Author:
Jia-qiang YANG
1
;
Fa-kun ZENG
1
;
Xuan YANG
2
;
Peng LI
1
Author Information
1. School of Pharmacy, Zunyi Medical College, Zunyi 563003, China
2. Chemistry Department, University of Manitoba, Winnipeg, MB, Canada, R3 T4 K6
- Publication Type:ORIGINAL ARTICLES
- Keywords:
phosphonate;
amino acid;
synthesis;
antitumor activity
- From:
Acta Pharmaceutica Sinica
2016;51(7):1105-
- CountryChina
- Language:Chinese
-
Abstract:
In search of effective anticancer agents, fifteen new phosphonate derivatives were designed and synthesized. Their structures were clearly established by elemental analysis, IR, 1H NMR and 13C NMR, and their antitumor activities were evaluated by MTT assay. Preliminary results in bioactivity tests indicated that some title compounds exhibited better activity. Among the active compounds, compounds 4e, 4n had better inhibition effect on A-549 cells growth with IC50 values of 8.7±0.8, 8.2±1.0 μmol·L-1, the IC50 values of compound 4c was 9.8±0.9 μmol·L-1 against SGC-7901 cells and compounds 4l, 4n exhibited more potent activities against EC-109 with IC50 values of 9.5±0.6, 9.4±0.5 μmol·L-1.
