DNA modifications by antitumor trans-[PtCl2(E-iminoether)(2)]

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Authors

ŽALUDOVÁ Renata ŽÁKOVSKÁ Alena KAŠPÁRKOVÁ Jana BALCAROVÁ Zdeňka VRÁNA Oldřich COLUCCIA Mauro NATILE Giovanni BRABEC Viktor

Year of publication 1997
Type Article in Periodical
Magazine / Source MOLECULAR PHARMACOLOGY
MU Faculty or unit

Faculty of Science

Citation
Field Pharmacology and pharmaceutical chemistry
Keywords INTERSTRAND CROSS-LINKS; ANTI-TUMOR ACTIVITY; PLATINUM COMPLEXES; IN-VITRO; CISPLATIN; BINDING; CIS-DIAMMINEDICHLOROPLATINUM(II); ADDUCTS; CYTOTOXICITY; ANTIBODIES
Description Recent findings that an analogue of clinically ineffective transplatin, trans-[PtCl2(E-iminoether)(2)], exhibits antitumor activity has helped reevaluation of the empirical structure-antitumor activity relationship generally accepted for platinum(II) complexes. According to this relationship, only the cis geometry of leaving ligands in the bifunctional platinum(II) complexes, should be therapeutically active. Global modifications of natural DNAs in cell-free media by trans-[PtCl2(E-iminoether)(2)] were studied through various molecular biophysical methods and compared with modifications by cis-[PtCl2(E-iminoether)(2)], transplatin, cisplatin, and monofunctional chlorodiethylenetriamineplatinum(II) chloride.

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