Citation: Xue-Jiao WU, Guang-Lin GOU, Xiao-Lan YANG, Jia-Qiang YANG. Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide[J]. Chinese Journal of Applied Chemistry, ;2021, 38(1): 36-43. doi: 10.19894/j.issn.1000-0518.200183 shu

Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide

School of Pharmacy, Zunyi Medical University, Zunyi 563000, China

Corresponding author: Jia-Qiang YANG, yjqcn@126.com
Received Date: 14 June 2020
Accepted Date: 18 September 2020

Fund Project: the Technology Department of Guizhou Province No.G[2014]7013

Figures(1)

In order to find antitumor compounds, fifteen dipeptide phosphonate derivatives(Ⅲa-Ⅲo) were designed and synthesized based on the phosphonate derivatives containing one amino acid fragment. Their antitumor activities in vitro were evaluated by the MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide) assay. The results show that the compounds inhibit the proliferation of the tumor cells. Among the active compounds, compound Ⅲf has better inhibition effect on A-549 (human lung cancer cells) and EC-109 (human esophageal cancer cells) growth with the half maximal inhibitory concentration (IC₅₀) values of (6.9±1.2) and (6.3±1.0) μmol/L, respectively, and compound Ⅲn shows more potent antitumor activities against SGC-7901(human gastric cancer cells) and EC-109 with the IC₅₀ values of (6.7±1.0) and (6.1±1.0) μmol/L, respectively, close to that of cisplatin.
- Dipeptide,
- Phosphonate,
- Antitumor activity
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