2-Benzoylpyridine- N(4)-tolyl thiosemicarbazones and their palladium(II) complexes: Cytotoxicity against leukemia cells

The palladium(II) complexes [Pd(2Bz4oT)Cl], [Pd(2Bz4mT)Cl], and [Pd(2Bz4pT)Cl] were prepared with N(4)- ortho- (H2Bz4oT) N(4)- meta- (H2Bz4mT) and N(4)- para- (H2Bz4pT) tolyl-thiosemicarbazones derived from 2-benzoylpyridine. The free thiosemicarbazones proved to be highly cytotoxic against Jurkat,...

Full description

Saved in:

Bibliographic Details
Published in:	Bioorganic & medicinal chemistry Vol. 17; no. 20; pp. 7138 - 7144
Main Authors:	Ferraz, Karina S.O., Ferandes, Lucas, Carrilho, Diego, Pinto, Mauro C.X., Leite, Maria de Fátima, Souza–Fagundes, Elaine M., Speziali, Nivaldo L., Mendes, Isolda C., Beraldo, Heloisa
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 15-10-2009 Elsevier
Subjects:	Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Cell Line, Tumor Crystallography, X-Ray Drug Screening Assays, Antitumor General aspects Humans Leukemia Leukemia - pathology Magnetic Resonance Spectroscopy Medical sciences Models, Molecular Palladium - chemistry Palladium(II) complexes Pharmacology. Drug treatments Thiosemicarbazones Thiosemicarbazones - chemistry Thiosemicarbazones - pharmacology Thiosemicarbazones Leukemia Palladium(II) complexes Antineoplastic agent Divalent metal Complexes Molecular structure Toxicity Liver Cytotoxicity Pyridine derivatives Hepatocyte T-Lymphocyte Tumor cell Human Promyelocytic leukemia Thiosemicarbazone Palladium II Complexes Organic ligand Transition metal Complexes X ray diffraction In vitro HL60 cell line Position isomer Cell line Platinoid Complexes Toluene derivatives Crystalline structure
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	The palladium(II) complexes [Pd(2Bz4oT)Cl], [Pd(2Bz4mT)Cl], and [Pd(2Bz4pT)Cl] were prepared with N(4)- ortho- (H2Bz4oT) N(4)- meta- (H2Bz4mT) and N(4)- para- (H2Bz4pT) tolyl-thiosemicarbazones derived from 2-benzoylpyridine. The free thiosemicarbazones proved to be highly cytotoxic against Jurkat, HL60 and the resistant HL60.Bcl-X L leukemia cell lines at nanomolar concentrations, but were much less cytotoxic to HepG2 human hepatoma cells. Upon coordination to palladium(II) the cytotoxic activity against all studied cell lines decreases. However, the high cytotoxicity of the free thiosemicarbazones against leukemia, together with their hepatotoxic profile similar to that of cisplatin suggest that N(4)-tolyl thiosemicarbazones have potential as chemotherapeutic drug candidates.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2009.08.063