Tuning of lipophilicity and cytotoxic potency by structural variation of anticancer platinum(IV) complexes

Author(s)
Michael Reithofer, Anna Bytzek, Seied Mojtaba Valiahdi, Christian Kowol, Michael Größl, Christian Hartinger, Michael Jakupec, Mathea Sophia Galanski, Bernhard Keppler
Abstract

A series of bis(carboxylato)dichlorido(ethane-1 2-diamine)platinum(IV) compounds with IC50 values ranging between 142 mu M and 18 nM was investigated with respect to their lipophilicity (by the shake flask method as well as microemulsion electrokinetic chromatography) reduction potential as well as their cellular accumulation in cancer cells in vitro In general the antiproliferative properties of the complexes correlated with their lipophilicity as well as their accumulation whereas differences in antiproliferative potency could not be explained by reduction potentials since they do not vary significantly within the investigated series of compounds Only minor effects for complexes featuring polar end groups were detected

Organisation(s)
Department of Inorganic Chemistry
Journal
Journal of Inorganic Biochemistry
Volume
105
Pages
46-51
No. of pages
6
ISSN
0162-0134
DOI
https://doi.org/10.1016/j.jinorgbio.2010.09.006
Publication date
2011
Peer reviewed
Yes
Austrian Fields of Science 2012
104003 Inorganic chemistry, 106002 Biochemistry
Sustainable Development Goals
SDG 3 - Good Health and Well-being
Portal url
https://ucrisportal.univie.ac.at/en/publications/ab93ba10-472d-4a70-b297-d595663726cd