Organometallic nucleoside analogues: effect of hydroxylalkyl linker length on cancer cell line toxicity
Research output: Contribution to journal › Article
A new series of chiral ferrocene derivatives containing both a hydroxyalkyl group and a thyminyl group on one cyclopentadienyl ring have been synthesised in order to probe structure activity relationships in cancer cell-line cytotoxicities. Stereoisomers of enantiomeric pairs of these so-called ferronucleosides have been studied and characterised by a combination of chiral analytical HPLC and single crystal X-Ray diffraction. Biological activity studies reveal that changing the length of the hydroxyalkyl group had marked effects on IC50 values, with compounds having shorter arms that more closely resemble endogenous nucleosides exhibiting lower cytotoxicities. Lipophilicities and electrochemical properties of this compound series have been studied in order to rationalise these trends and indicate future directions of study.
|Number of pages||11|
|Journal||European Journal of Inorganic Chemistry|
|Early online date||17 Oct 2016|
|Publication status||Published - 10 Jan 2017|