Synthesis, characterization and biological activity of 5-fluorouracil derivatives of rare earth (Gd, Dy, Er) substituted phosphotungstate

Xia Liu; Qiang Gan; Changgen Feng

doi:10.1016/j.ica.2015.11.034

Synthesis, characterization and biological activity of 5-fluorouracil derivatives of rare earth (Gd, Dy, Er) substituted phosphotungstate

Xia Liu^*
, Qiang Gan
, Changgen Feng

^*Corresponding author for this work

School of Mechatronical Engineering

China Agricultural University
Beijing Institute of Technology

Research output: Contribution to journal › Article › peer-review

11 Citations (Scopus)

Abstract

Three new rare earth (Gd, Dy, Er) substituted phosphotungstates containing 5-fluorouracil, K₁₀C₄H₄FN₂O₂Gd(PW₁₁O₃₉)₂·8H₂O, K₁₀C₄H₄FN₂O₂Dy(PW₁₁O₃₉)₂·9H₂O and K₉(C₄H₄FN₂O₂)₂Er(PW₁₁O₃₉)₂·10H₂O, were synthesized by degradation method and self-assembly method. Analytical results demonstrated that the Keggin polyanion and the pyrimidine ring of 5-FU were maintained in its structures, and TG test shown compounds have good thermostability. MTT assay was used to measure its antitumor activity against HeLa and HepG-2 cells, and their cytotoxicity toward HEK293 cell. Results show that the IC₅₀ of title compounds against HeLa and HepG-2 tumor cells are 7.14, 6.16, 5.95 μmol L^-1 and 5.62, 5.96, 6.88 μmol L^-1, respectively. And their antitumor activity are superior to rare earth substituted phosphotungstates K₁₁Gd(PW₁₁O₃₉)₂·15H₂O, K₁₁Dy(PW₁₁O₃₉)₂·10H₂O, K₁₁Er(PW₁₁O₃₉)₂·10H₂O and 5-fluorouracil. Which suggests title compounds have excellent antitumor activity due to the synergistic effect between 5-fluorouracil group, rare earth ions and Keggin polyanions.

Original language	English
Pages (from-to)	299-303
Number of pages	5
Journal	Inorganica Chimica Acta
Volume	450
DOIs	https://doi.org/10.1016/j.ica.2015.11.034
Publication status	Published - 24 Aug 2016

Keywords

5-Fluorouracil
Antitumor
POMs
Rare earth

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10.1016/j.ica.2015.11.034

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@article{e09d76e65cac4b39bae9e243e3a8a26f,

title = "Synthesis, characterization and biological activity of 5-fluorouracil derivatives of rare earth (Gd, Dy, Er) substituted phosphotungstate",

abstract = "Three new rare earth (Gd, Dy, Er) substituted phosphotungstates containing 5-fluorouracil, K10C4H4FN2O2Gd(PW11O39)2·8H2O, K10C4H4FN2O2Dy(PW11O39)2·9H2O and K9(C4H4FN2O2)2Er(PW11O39)2·10H2O, were synthesized by degradation method and self-assembly method. Analytical results demonstrated that the Keggin polyanion and the pyrimidine ring of 5-FU were maintained in its structures, and TG test shown compounds have good thermostability. MTT assay was used to measure its antitumor activity against HeLa and HepG-2 cells, and their cytotoxicity toward HEK293 cell. Results show that the IC50 of title compounds against HeLa and HepG-2 tumor cells are 7.14, 6.16, 5.95 μmol L-1 and 5.62, 5.96, 6.88 μmol L-1, respectively. And their antitumor activity are superior to rare earth substituted phosphotungstates K11Gd(PW11O39)2·15H2O, K11Dy(PW11O39)2·10H2O, K11Er(PW11O39)2·10H2O and 5-fluorouracil. Which suggests title compounds have excellent antitumor activity due to the synergistic effect between 5-fluorouracil group, rare earth ions and Keggin polyanions.",

keywords = "5-Fluorouracil, Antitumor, POMs, Rare earth",

author = "Xia Liu and Qiang Gan and Changgen Feng",

note = "Publisher Copyright: {\textcopyright} 2016 Published by Elsevier B.V.",

year = "2016",

month = aug,

day = "24",

doi = "10.1016/j.ica.2015.11.034",

language = "English",

volume = "450",

pages = "299--303",

journal = "Inorganica Chimica Acta",

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publisher = "Elsevier B.V.",

}

TY - JOUR

T1 - Synthesis, characterization and biological activity of 5-fluorouracil derivatives of rare earth (Gd, Dy, Er) substituted phosphotungstate

AU - Liu, Xia

AU - Gan, Qiang

AU - Feng, Changgen

PY - 2016/8/24

Y1 - 2016/8/24

N2 - Three new rare earth (Gd, Dy, Er) substituted phosphotungstates containing 5-fluorouracil, K10C4H4FN2O2Gd(PW11O39)2·8H2O, K10C4H4FN2O2Dy(PW11O39)2·9H2O and K9(C4H4FN2O2)2Er(PW11O39)2·10H2O, were synthesized by degradation method and self-assembly method. Analytical results demonstrated that the Keggin polyanion and the pyrimidine ring of 5-FU were maintained in its structures, and TG test shown compounds have good thermostability. MTT assay was used to measure its antitumor activity against HeLa and HepG-2 cells, and their cytotoxicity toward HEK293 cell. Results show that the IC50 of title compounds against HeLa and HepG-2 tumor cells are 7.14, 6.16, 5.95 μmol L-1 and 5.62, 5.96, 6.88 μmol L-1, respectively. And their antitumor activity are superior to rare earth substituted phosphotungstates K11Gd(PW11O39)2·15H2O, K11Dy(PW11O39)2·10H2O, K11Er(PW11O39)2·10H2O and 5-fluorouracil. Which suggests title compounds have excellent antitumor activity due to the synergistic effect between 5-fluorouracil group, rare earth ions and Keggin polyanions.

AB - Three new rare earth (Gd, Dy, Er) substituted phosphotungstates containing 5-fluorouracil, K10C4H4FN2O2Gd(PW11O39)2·8H2O, K10C4H4FN2O2Dy(PW11O39)2·9H2O and K9(C4H4FN2O2)2Er(PW11O39)2·10H2O, were synthesized by degradation method and self-assembly method. Analytical results demonstrated that the Keggin polyanion and the pyrimidine ring of 5-FU were maintained in its structures, and TG test shown compounds have good thermostability. MTT assay was used to measure its antitumor activity against HeLa and HepG-2 cells, and their cytotoxicity toward HEK293 cell. Results show that the IC50 of title compounds against HeLa and HepG-2 tumor cells are 7.14, 6.16, 5.95 μmol L-1 and 5.62, 5.96, 6.88 μmol L-1, respectively. And their antitumor activity are superior to rare earth substituted phosphotungstates K11Gd(PW11O39)2·15H2O, K11Dy(PW11O39)2·10H2O, K11Er(PW11O39)2·10H2O and 5-fluorouracil. Which suggests title compounds have excellent antitumor activity due to the synergistic effect between 5-fluorouracil group, rare earth ions and Keggin polyanions.

KW - 5-Fluorouracil

KW - Antitumor

KW - POMs

KW - Rare earth

UR - https://www.scopus.com/pages/publications/84975090483

U2 - 10.1016/j.ica.2015.11.034

DO - 10.1016/j.ica.2015.11.034

M3 - Article

AN - SCOPUS:84975090483

SN - 0020-1693

VL - 450

SP - 299

EP - 303

JO - Inorganica Chimica Acta

JF - Inorganica Chimica Acta

ER -

Synthesis, characterization and biological activity of 5-fluorouracil derivatives of rare earth (Gd, Dy, Er) substituted phosphotungstate

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Keywords

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