Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide

doi:10.19894/j.issn.1000-0518.200183

Chinese Journal of Applied Chemistry ›› 2021, Vol. 38 ›› Issue (1): 36-43.DOI: 10.19894/j.issn.1000-0518.200183

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Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide

WU Xue-Jiao, GOU Guang-Lin, YANG Xiao-Lan, YANG Jia-Qiang^*

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

Received:2020-06-14 Revised:2020-09-18 Published:2021-01-01 Online:2021-02-01
Supported by:
Technology Department of Guizhou Province(No.G[2014]7013)

Abstract

Abstract: 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.

Key words: Dipeptide, Phosphonate, Antitumor activity

CLC Number:

O626.2

WU Xue-Jiao, GOU Guang-Lin, YANG Xiao-Lan, YANG Jia-Qiang. Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide[J]. Chinese Journal of Applied Chemistry, 2021, 38(1): 36-43.

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Synthesis and Antitumor Activity of Phosphonate Derivatives Containing Dipeptide

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