Mono-nuclear cis-Pd(II) chloride complex of the thio-nucleotide analogue 5-methyl-thiouracil and its biological activity
The new palladium(II) complex cis-Cl-[PdCl2(TPP)(MTUC)]·3(H2O) (MTUC=6-methyl-thiouracil and TPP=triphenylphosphine) was evaluated for its in vitro cytotoxicity against MCF-7 (breast) and HeLa (cervical) cancer cell lines. The binding affinity of 1 towards DNA and lipoxygenase was also studied. Part...
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| Published in: | Polyhedron Vol. 87; pp. 251 - 258 |
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| Abstract | The new palladium(II) complex cis-Cl-[PdCl2(TPP)(MTUC)]·3(H2O) (MTUC=6-methyl-thiouracil and TPP=triphenylphosphine) was evaluated for its in vitro cytotoxicity against MCF-7 (breast) and HeLa (cervical) cancer cell lines. The binding affinity of 1 towards DNA and lipoxygenase was also studied. Partial least squares regression analysis correlates the variation of the IC50 values with the variations of energetic parameters of 1 and related palladium(II) complexes.
The new mixed ligand palladium(II) complex of formula cis-Cl-[PdCl2(TPP)(MTUC)]·3(H2O) (1) was obtained by reacting 6-methyl-thiouracil (MTUC) with triphenylphosphine (TPP). The complex was characterized by vibrational spectroscopy (FT-IR), 1H NMR, UV–Vis spectroscopic techniques and its structure was confirmed by X-ray crystallography. Mixed ligand complexes of palladium(II) dichloride with thiones and phosphines are very rare in the literature. Compound 1 is the fourth of this kind of compounds which has also been examined for its biological effects.
Complex 1 was evaluated for its in vitro cytotoxic activity (cell viability) against human cancer cell lines: MCF-7 (breast) and HeLa (cervical) with tryban blue assay. The results showed that 1 mediates a mild cytotoxic response to the tested cancer cell lines. The binding affinity of 1 towards the intracellular molecules DNA and lipoxygenase (LOX) was studied for the evaluation of the mechanism of its cytotoxicity. Partial least squares (PLS) regression analysis was carried out to correlate the variation of the IC50 values (Y-variables) with the variations of energetic parameters (X-variables), calculated from molecular docking calculation for 1 and related palladium(II) complexes reported. |
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| AbstractList | The new palladium(II) complex cis-Cl-[PdCl2(TPP)(MTUC)]·3(H2O) (MTUC=6-methyl-thiouracil and TPP=triphenylphosphine) was evaluated for its in vitro cytotoxicity against MCF-7 (breast) and HeLa (cervical) cancer cell lines. The binding affinity of 1 towards DNA and lipoxygenase was also studied. Partial least squares regression analysis correlates the variation of the IC50 values with the variations of energetic parameters of 1 and related palladium(II) complexes.
The new mixed ligand palladium(II) complex of formula cis-Cl-[PdCl2(TPP)(MTUC)]·3(H2O) (1) was obtained by reacting 6-methyl-thiouracil (MTUC) with triphenylphosphine (TPP). The complex was characterized by vibrational spectroscopy (FT-IR), 1H NMR, UV–Vis spectroscopic techniques and its structure was confirmed by X-ray crystallography. Mixed ligand complexes of palladium(II) dichloride with thiones and phosphines are very rare in the literature. Compound 1 is the fourth of this kind of compounds which has also been examined for its biological effects.
Complex 1 was evaluated for its in vitro cytotoxic activity (cell viability) against human cancer cell lines: MCF-7 (breast) and HeLa (cervical) with tryban blue assay. The results showed that 1 mediates a mild cytotoxic response to the tested cancer cell lines. The binding affinity of 1 towards the intracellular molecules DNA and lipoxygenase (LOX) was studied for the evaluation of the mechanism of its cytotoxicity. Partial least squares (PLS) regression analysis was carried out to correlate the variation of the IC50 values (Y-variables) with the variations of energetic parameters (X-variables), calculated from molecular docking calculation for 1 and related palladium(II) complexes reported. |
| Author | Kourkoumelis, N. Charalampou, D.C. Hadjiliadis, N. Owczarzak, A.M. Hadjikakou, S.K. Banti, C.N. Kubicki, M. |
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| CitedBy_id | crossref_primary_10_1080_00958972_2016_1241394 crossref_primary_10_1016_j_jinorgbio_2017_11_004 crossref_primary_10_1515_mgmc_2022_0016 crossref_primary_10_1016_j_ccr_2016_02_001 crossref_primary_10_1016_j_ica_2015_08_031 crossref_primary_10_1002_slct_201900707 crossref_primary_10_3389_fchbi_2024_1338630 crossref_primary_10_1016_j_ejmech_2017_10_067 crossref_primary_10_1080_07391102_2017_1318304 |
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| Keywords | Psllsdium metallotherapeutics Molecular modeling Cell studies CT-DNA and Lipoxygenase PCA |
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| SubjectTerms | Cell studies CT-DNA and Lipoxygenase Molecular modeling PCA Psllsdium metallotherapeutics |
| Title | Mono-nuclear cis-Pd(II) chloride complex of the thio-nucleotide analogue 5-methyl-thiouracil and its biological activity |
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