期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 17, 期 20, 页码 7138-7144出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.08.063
关键词
Thiosemicarbazones; Palladium(II) complexes; Leukemia
资金
- Fapemig
- CNPq
- INCT-INOFAR/CNPq [573.564/2008-6]
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. (C) 2009 Elsevier Ltd. All rights reserved.
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