Effects of a piperidine ligand on DNA modification by antitumor cisplatin analogues

0126968 - BFU-R 20033049 RIV US eng J - Journal Article
Kašpárková, Jana - Nováková, Olga - Najajreh, Y. - Gibson, D. - Perez, J.M. - Brabec, Viktor
Effects of a piperidine ligand on DNA modification by antitumor cisplatin analogues.
Chemical Research in Toxicology. Roč. 16, č. 11 (2003), s. 1424-1432. ISSN 0893-228X. E-ISSN 1520-5010
R&D Projects: GA ČR GA305/02/1552; GA AV ČR KJB5004301; GA AV ČR IBS5004009
Institutional research plan: CEZ:AV0Z5004920
Keywords : DNA * piperidine ligand * antitumor cisplatin analogues
Subject RIV: BO - Biophysics
Impact factor: 3.332, year: 2003

Replacement of the ammine group in antitumor cisplatin by a heterocyclic ligand (piperidine, piperazine, or 4-picoline) results in reduction of cytotoxicity in human ovarian cancer cells. The results suggest that in certain cancer cells the lower cytotoxicity of cis-[PtCl2(NH3)(piperidine)] might be partially associated with reduced affinity of the high mobility group proteins to the major intrastrand cross-links of this analogue relative to the same adducts of cisplatin. The results support the view that the concept based on the design of the complexes structurally derived from cisplatin that do not present an altered DNA binding mode may be less effective in the search for new platinum drugs that would overcome cisplatin resistance.
Permanent Link: http://hdl.handle.net/11104/0025195