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Relevance of the leaving group for antitumor activity of new platinum(II) compounds containing anthracene derivatives as a carrier ligand.

Abstract：

:A new anticancer-active platinum(II) compound [Pt(A9pyp)(dmso)(cbdca)], containing the E-1-(9-anthryl)-3-(2-pyridyl)-2-propenone ligand (abbreviated as A9pyp) has been synthesized by the replacement of the anionic chloride ligands in cis-[Pt(A9pyp)(dmso)Cl(2)] by the dianionic chelating cyclobutanedicarboxylate ligand (abbreviated as cbdca). The in vitro relevance of the leaving group of these new platinum(II) compounds has been investigated. Measurements of the time-dependent intracellular accumulation of both compounds in human ovarian carcinoma cell lines show that the leaving group affects their cellular uptake. In addition, the leaving group also influences DNA platination, and, therefore, has an effect on the biological activity against a pair of human ovarian carcinoma cell lines, i.e. sensitive and resistant to cisplatin.

journal_name

J Inorg Biochem

journal_title

Journal of inorganic biochemistry

authors

Marqués-Gallego P,Contaldi S,den Dulk H,Monari M,Brouwer J,Jaehde U,Kalayda GV,Reedijk J

doi

10.1016/j.jinorgbio.2009.08.009

subject

Has Abstract

pub_date

2009-12-01 00:00:00

pages

1602-8

issue

12

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(09)00198-6

journal_volume

103

pub_type

杂志文章

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