| Autor: |
Green BP; School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia. trevor.hambley@sydney.edu.au., Renfrew AK, Glenister A, Turner P, Hambley TW |
| Jazyk: |
angličtina |
| Zdroj: |
Dalton transactions (Cambridge, England : 2003) [Dalton Trans] 2017 Nov 21; Vol. 46 (45), pp. 15897-15907. |
| DOI: |
10.1039/c7dt03645k |
| Abstrakt: |
Cobalt(iii) chaperones are a promising class of bioreductive prodrugs under investigation for the delivery of cytotoxic ligands to hypoxic solid tumours. Here we investigate a series of cobalt complexes as chaperones for hydroxamic acid ligands, comparing the properties of the cyclic cyclen (1,4,7,10-tetraazacyclododecane) ancillary ligand with the tripodal tpa (tris-(2-pyridylmethyl)amine) and tren (tris-(2-aminoethyl)amine). A small library of complexes containing several different hydroxamic acids, including the MMP inhibitor Marimistat and the fluorescent ligand C343haH 2 , were prepared and their pK a values, reduction potentials, and in some cases X-ray crystal structures, were determined. The antiproliferative actitivity of the series was evaluated against DLD-1 colon cancer cells and the cellular accumulation of the fluorescent C343haH 2 complexes was monitored by ICPMS and confocal fluorescence microscopy, revealing that the nature of the ancillary ligand significantly influences the complexes' properties, cytotoxicity and cellular distribution. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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