Abstract
The palladium(II) bis-chelate complexes of the type [Pd(TSC1−5)2] (6–10), with their corresponding ligands 4-phenyl-1-(acetone)-
thiosemicarbazone, HTSC1 (1), 4-phenyl-1-(2
-chloro-benzaldehyde)-thiosemicarbazone, HTSC2 (2), 4-phenyl-1-(3
-hydroxybenzaldehyde)-thiosemicarbazone, HTSC3 (3), 4-phenyl-1-(2
-naphthaldehyde)-thiosemicarbazone, HTSC4 (4), and 4-phenyl1-(1
-nitro-2
-naphthaldehyde)-thiosemicarbazone, HTSC5 (5), were synthesized and characterized by elemental analysis and
spectroscopic techniques (IR and 1
H- and 13C-NMR). The molecular structure of HTSC3
, HTSC4
, and [Pd(TSC1
)2] (6) have been
determined by single crystal X-ray crystallography. Complex 6 shows a square planar geometry with two deprotonated ligands
coordinated to PdII through the azomethine nitrogen and thione sulfur atoms in a cis arrangement. The in vitro cytotoxic activity
measurements indicate that the palladium(II) complexes (IC50 = 0.01–9.87 𝜇M) exhibited higher antiproliferative activity than
their free ligands (IC50 = 23.48–70.86 and >250 𝜇M) against different types of human tumor cell lines. Among all the studied
palladium(II) complexes, the [Pd(TSC3
)2] (8) complex exhibited high antitumor activity on the DU145 prostate carcinoma and
K562 chronic myelogenous leukemia cells, with low values of the inhibitory concentration (0.01 and 0.02 𝜇M, resp.).
thiosemicarbazone, HTSC1 (1), 4-phenyl-1-(2
-chloro-benzaldehyde)-thiosemicarbazone, HTSC2 (2), 4-phenyl-1-(3
-hydroxybenzaldehyde)-thiosemicarbazone, HTSC3 (3), 4-phenyl-1-(2
-naphthaldehyde)-thiosemicarbazone, HTSC4 (4), and 4-phenyl1-(1
-nitro-2
-naphthaldehyde)-thiosemicarbazone, HTSC5 (5), were synthesized and characterized by elemental analysis and
spectroscopic techniques (IR and 1
H- and 13C-NMR). The molecular structure of HTSC3
, HTSC4
, and [Pd(TSC1
)2] (6) have been
determined by single crystal X-ray crystallography. Complex 6 shows a square planar geometry with two deprotonated ligands
coordinated to PdII through the azomethine nitrogen and thione sulfur atoms in a cis arrangement. The in vitro cytotoxic activity
measurements indicate that the palladium(II) complexes (IC50 = 0.01–9.87 𝜇M) exhibited higher antiproliferative activity than
their free ligands (IC50 = 23.48–70.86 and >250 𝜇M) against different types of human tumor cell lines. Among all the studied
palladium(II) complexes, the [Pd(TSC3
)2] (8) complex exhibited high antitumor activity on the DU145 prostate carcinoma and
K562 chronic myelogenous leukemia cells, with low values of the inhibitory concentration (0.01 and 0.02 𝜇M, resp.).
| Translated title of the contribution | Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines: Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines |
|---|---|
| Original language | American English |
| Pages (from-to) | 1-12 |
| Number of pages | 12 |
| Journal | Bioinorganic Chemistry and Applications |
| DOIs | |
| State | Published - 1 Jan 2015 |