Synthesis, characterization, and in vitro cytotoxic activities of benzaldehyde thiosemicarbazone derivatives and their palladium(II) and platinum(II) complexes against various human tumor cell lines

The palladium (II) bis-chelate Pd (L 1 - 3) 2 and platinum (II) tetranuclear Pt 4 (L 4) 4 complexes of benzaldehyde thiosemicarbazone derivatives have been synthesized, and characterized by elemental analysis and IR, FAB (+) -mass and NMR (1 H, 13 C) spectroscopy. The complex Pd (L 2) 2 [H L 2 = m -CN-benzaldehyde thiosemicarbazone] shows a square-planar geometry with two deprotonated ligands (L) coordinated to Pd II through the nitrogen and sulphur atoms in a transarrangement, while the complex Pt 4 (L 4) 4 [H L 4 = 4 -phenyl-1-benzaldehyde thiosemicarbazone] has a tetranuclear geometry with four tridentate ligands coordinated to four Pt II ions through the carbon (aromatic ring), nitrogen, and sulphur atoms where the ligands are deprotonated at the NH group. The in vitro antitumor activity of the ligands and their complexes was determined against different human tumor cell lines, which revealed that the palladium (II) and platinum (II) complexes are more cytotoxic than their ligands with IC 50 values at the range of 0.07-3.67 µM. The tetranuclear complex Pt 4 (L 4) 4, with the phenyl group in the terminal amine of the ligand, showed higher antiproliferative activity (CI 50 = 0.07-0.12 µM) than the other tested palladium (II) complexes

Synthesis and Characterization of New Palladium(II) Complexes with Ligands Derived from Furan-2-carbaldehyde and Benzaldehyde Thiosemicarbazone and their in vitro Cytotoxic Activities against Various Human Tumor Cell Lines

With the ligands 4-phenyl-1-(furan-2-carbaldehyde)thiosemicarbazone, HTSC1, (1), 4-phenyl-1- (5 -phenyl-furan-2-carbaldehyde)thiosemicarbazone, HTSC2 (2), o-methoxy-benzaldehydethiosemicarbazone, HTSC3 (3), and o-cyano-benzaldehydethiosemicarbazone, HTSC4 (4), the corresponding palladium(II) complexes, Pd(TSC1)2 (5), Pd(TSC2)2 (6), Pd(TSC3)2 (7), and Pd(TSC4)2 (8) were synthesized and characterized by elemental analysis and spectroscopic techniques. The crystal structure of Pd(TSC3)2 (7) was determined by single-crystal X-ray diffraction. Complex 7 shows a squareplanar geometry, where two deprotonated ligands are coordinated to the PdII center through the nitrogen and sulfur atoms in a trans arrangement. In vitro antitumor studies against different human tumor cell lines have revealed that the palladium(II) complexes 5– 8 are more cytotoxic (IC50 values in the range of 0.21 – 3.79 µM) than their corresponding ligands (1 – 4) (> 60 µM). These results indicate that the antiproliferative activity is enhanced when thiosemicarbazone ligands are coordinated to the metal. Among the studied palladium(II) complexes, 8 exhibits high antitumor activity on K562 chronic myelogenous leukemia cells with a low value of the inhibitory concentration (IC50 = 0.21 µM)

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

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'-hydroxy-benzaldehyde)-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 through the azomethine nitrogen and thione sulfur atoms in a cis arrangement. The in vitro cytotoxic activity measurements indicate that the palladium(II) complexes (–9.87¿M) exhibited higher antiproliferative activity than their free ligands (–70.86 and >250¿M) 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¿M, resp.)

Estudio químico de la alga roja

Analiza la composición química de un alga de la clase Rhodophyceae, que abunda en el litoral peruano, la Grateloupia doyphora, con la intención de difundir su empleo, ya que representa una buena fuente proteica que podría contribuir a solucionar en algo los problemas de deficiencia nutricional, especialmente en los sectores de nuestra población que se ven más afectados

Estudio químico de la alga roja

No presenta resumen

Nuevos materiales bioinorgánicos de actividad antitumoral

Los compuestos orgánicos derivados de las tiosemicarbazonas (R1R2-C=N-NH-C(S)-NHR) cumplen un rol importante en la química medicinal debido a sus aplicaciones farmacológicas. Basada en esta comprobación, la investigación describe la síntesis, caracterización y evaluación de la actividad antitumoral in vitro de nuevos compuestos orgánicos derivados del 4-R-1-(3´/5´-X-fenil-3´/5´- carboxaldehído isoxazol) tiosemicarbazona (R=H, Ph; X=F, Cl, OCH3, CH3).Los compuestos orgánicos derivados de las tiosemicarbazonas (R1R2-C=N-NH-C(S)-NHR) cumplen un rol importante en la química medicinal debido a sus aplicaciones farmacológicas. Basada en esta comprobación, la investigación describe la síntesis, caracterización y evaluación de la actividad antitumoral in vitro de nuevos compuestos orgánicos derivados del 4-R-1-(3´/5´-X-fenil-3´/5´- carboxaldehído isoxazol) tiosemicarbazona (R=H, Ph; X=F, Cl, OCH3, CH3)

Materiales bioinorgánicos de paladio con compuestos orgánicos derivados de la tiosemicarbazona de actividad antitumoral

El presente trabajo informa acerca de la preparación, caracterización y actividad anti tu moral de nuevos compuestos orgánicos (ligantes) del tipo tiosemicarbazona, RCH=N-NHC(S)-NH2 [R=pirrol-2-carboxaldehído y tiofeno 2-carboxaldehído] y sus complejos me tálicos de paladio(II). El análisis elemental y las técnicas espectroscópicas de infrarrojo y resonancia magnética nuclear de protón y carbono revelan que los ligantes tiosemicarbazonas están desprotonados y se encuentran enlazados al centro metálico a través de dos áto mos de nitrógeno (N) y azufre (S) en una configuración trans