Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines

Wilfredo Román Hernandez Gorritti, Juan Paz Castillo Berríos, Fernando Carlos Carrasco Solis, Abraham J. Vaisberg, Evgenia Spodine, Jorge Manzur, Lothar Hennig, Steffen Blaurock, Lothar Beyer

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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-phenyl-
1-(1󸀠-nitro-2󸀠-naphthaldehyde)-thiosemicarbazone, HTSC5 (5), were synthesized and characterized by elemental analysis and
spectroscopic techniques (IR and 1H- 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 contributionSíntesis y caracterización de nuevos complejos de platino(II) con tiosemicarbazonas y sus actividades citotóxicas frente a varias líneas celulares tumorales de humano
Original languageAmerican English
Article numberID 524701
Number of pages12
JournalBioinorganic Chemistry and Applications
Volume2013
Issue numberID 524701
DOIs
StatePublished - 3 Oct 2013

COAR

  • Article

Ulima Repository Category

  • Ciencias / Química

Ulima Repository Subject

  • Cell line, Tumor
  • In vitro techniques
  • Línea celular tumoral
  • Paladio
  • Palladium
  • Thiosemicarbazones
  • Tiosemicarbazonas
  • Técnicas in vitro

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