Metal complexes of 3-(4-bromophenyl)-1-pyridin-2-ylprop- 2-en-1-one thiosemicarbazone: cytotoxic activity and investigation on the mode of action of the gold(III) complex
作者： Luciana B. P. Sâmia , Gabrieli L. Parrilha , Jeferson G. Da Silva , Jonas P. Ramos , Elaine M. Souza-Fagundes
DOI: 10.1007/S10534-016-9933-5
关键词: Topoisomerase 、 Thioredoxin reductase 、 Cytotoxic T cell 、 Active site 、 Stereochemistry 、 Chalcone 、 Chemistry 、 Monocytic leukemia 、 Structure–activity relationship 、 Semicarbazone
摘要: Complexes [Au(PyCT4BrPh)Cl]Cl (1), [Pt(PyCT4BrPh)Cl]0.5KCl (2), and [Pd(PyCT4BrPh)Cl]KCl (3) were obtained with 3-(4-bromophenyl)-1-pyridin-2-ylprop-2-en-1-one thiosemicarbazone (HPyCT4BrPh). Although complexes (2) did not exhibit potent cytotoxic activity, HPyCT4BrPh its gold(III) complex (1) proved to be highly against HL-60 (human promyelocytic leukemia) THP-1 monocytic cells, MDA-MB 231 MCF-7 breast adenocarcinoma) solid tumor cells. Except for upon coordination a 2- 3-fold increase in the effect was observed. An investigation on possible biological targets of carried out. Complex but free inhibits enzymatic activity thioredoxin reductase (TrxR). The affinity 1 TrxR suggests metal binding selenol residue active site enzyme. While inactive, able inhibit topoisomerase IB (Topo IB) activity. Hence, inhibition Topo could contribute mechanism action (1).
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