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
N1 - Publisher Copyright:
© 2016 Published by Elsevier B.V.
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 - http://www.scopus.com/inward/record.url?scp=84975090483&partnerID=8YFLogxK
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 -