21198-48-1Relevant articles and documents
Effect of Structural Modifications to Glyoxal-bis(thiosemicarbazonato)copper(II) Complexes on Cellular Copper Uptake, Copper-Mediated ATP7A Trafficking, and P-Glycoprotein Mediated Efflux
Acevedo, Karla M.,Hayne, David J.,McInnes, Lachlan E.,Noor, Asif,Duncan, Clare,Moujalled, Diane,Volitakis, Irene,Rigopoulos, Angela,Barnham, Kevin J.,Villemagne, Victor L.,White, Anthony R.,Donnelly, Paul S.
, p. 711 - 723 (2018)
Bis(thiosemicarbazonato)copper(II) complexes are of interest as potential therapeutics for cancer and neurodegenerative diseases as well as imaging agents for positron emission tomography (PET). The cellular uptake of six bis(thiosemcarbazonato)copper(II)complexes derived from glyoxal, with different functional groups Cu(gtsx) where x = different functional groups, was investigated in SKOV-3, HEK293, and HEK293 P-gp cell lines. Treatment of the cells with the copper complexes increased intracellular copper and increased levels of p-ERK due to activation of the Ras-Raf-MEK-ERK pathway. Treatment of SKOV-3 cells with low concentrations (μM) of two of the copper complexes led to trafficking of the endogenous copper transporter ATP7A from the Golgi network to the cell membrane. Experiments in HEK293 and HEK293-P-gp cells suggest that Cu(gtsm) and Cu(gtse) are substrates for the P-gp efflux protein but the complex with a pyrrolidine functional group, Cu(gtspyr), is not. A PET experiment in mice showed that [64Cu]Cu(gtspyr) has reasonable brain uptake but high liver uptake.
Copper compound taking 2-thiophenecarboxaldehyde thiosemicarbazone as ligand and synthesis method of copper compound
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Paragraph 0046-0051, (2020/03/06)
The invention discloses a copper compound taking 2-thiophenecarboxaldehyde thiosemicarbazone as a ligand and a synthesis method of the copper compound. The synthesis method comprises the following steps: adding thiosemicarbazone into absolute ethyl alcohol, performing stirring and dissolution, adding 2-thiophenecarboxaldehyde, performing uniform mixing, stirring the mixed solution at 70 DEG C in awater bath, performing volatilization at room temperature, separating a crystal so as to obtain a ligand; and adding the prepared ligand into absolute ethyl alcohol, performing stirring and dissolving, adding CuBr2.2H2O after dissolution, performing stirring at 70 DEG C in a water bath, performing volatilization at room temperature, and separating out a crystal, so as to obtain a Cu compound of the ligand. An in-vitro proliferation inhibition activity experiment is further carried out on the synthesized copper compound, results show that the synthesized series of copper compounds have generally good in-vitro activity, particularly have high specificity on human T24 and HeLa cells, show good inhibitory activity, have little toxic effect on human normal cells, and are suitable for preparingefficient and low-toxicity anti-tumor drugs.
Synthesis, characterization and biological evaluation of novel 1-N-substituted thiocarbomoyl-3-ferrocenyl-2-pyrazoline derivatives
Parveen, Humaira,Alatawi, Raedah Aiyed Suliman,Khan, Salman Ahmad,Al-Ahmdi, Mohammed Issa,Mukhtar, Sayeed,Azam, Amir,Elsayed, Nadia H.
, p. 1835 - 1840 (2016/07/06)
Some novel 1-N-substituted thiocarbomoyl-3-ferrocenyl-2-pyrazoline derivatives were synthesized and evaluated for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. The results showed that most of the compounds exhibited promising activity (IC50 values in the range of 0.050-1.683 μM) than the reference drug metronidazole (IC50 = 1.78 μM). Active compounds were further screened for cytotoxicity against human embryonic kidney-293 (HEK-293) normal cell lines to ensure their toxic effect and the results revealed that active compounds were least toxic in the concentration range of 2.5-50 μM for 48 h and 2.5-25 μM for 72 h. At 100 μM for 48 h and at 50 μM for 72 h only four compounds 2c, 2h, 2k and 2l showed maximum viability and least cytotoxicity, respectively, concluding that all the screened compounds were least cytotoxic against human embryonic kidney-293 (HEK-293) normal cell lines in the concentration range of 2.5-50 and 2.5-25 μM.
