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, HL60 and the resistant HL60.Bcl-X(L) leukemia cell lines at nanomolar concentrations, but were much less cytotoxic to HepG2human 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.
Departamento de Química, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, Brazil.
Karina S O
KS
Ferraz
Lucas
L
Ferandes
Diego
D
Carrilho
Mauro C X
MC
Pinto
Maria de Fátima
Mde F
Leite
Elaine M
EM
Souza-Fagundes
Nivaldo L
NL
Speziali
Isolda C
IC
Mendes
Heloisa
H
Beraldo
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007938:Leukemia / Q000473:pathology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D010165:Palladium / Q000737:chemistry*; D013882:Thiosemicarbazones / Q000737:chemistry / Q000494:pharmacology*
C541531:2-benzoylpyridine N(4)-methylthiosemicarbazone; D000970:Antineoplastic Agents; D013882:Thiosemicarbazones; D010165:Palladium