CYTOTOXICITY AND ANTITUMOR-ACTIVITY OF PLATINUM(II) COMPLEXES OF AROMATIC AND CYCLOALKANECARBOXYLIC ACID HYDRAZIDES

Citation
Dn. Kushev et al., CYTOTOXICITY AND ANTITUMOR-ACTIVITY OF PLATINUM(II) COMPLEXES OF AROMATIC AND CYCLOALKANECARBOXYLIC ACID HYDRAZIDES, Zeitschrift fur Naturforschung. C, A journal of biosciences, 52(1-2), 1997, pp. 49-54
Citations number
12
Categorie Soggetti
Biology
ISSN journal
09395075
Volume
52
Issue
1-2
Year of publication
1997
Pages
49 - 54
Database
ISI
SICI code
0939-5075(1997)52:1-2<49:CAAOPC>2.0.ZU;2-Y
Abstract
New platinum(II) complexes of cyclohexanecarboxylic acid hydrazide (ch cah) were synthesized and characterized by elemental analysis, IR, and H-1 NMR spectra. Their inhibitor Si effects on cell growth and macrom olecular synthesis of Friend leukemia cells in culture as well as the in vivo antitumor activity towards L1210 leukemia in mice were compare d with those of complexes containing differently substituted aromatic acid hydrazides. Some of the complexes exhibited antineoplastic activi ty. No correlation between the in vitro cytotoxicity and the in vivo a ntitumor activity was found. However, there was a relationship between the in vitro macromolecular synthesis inhibition profile and the in v ivo antineoplastic effect, similar to that of cisplatin. On the other hand, only agents containing one ammine ligand were active in vivo. Th e substitution of the aromatic ring by a cycloalkane residue increased significantly the antitumor effect, with [Pt(NH3)(chcah)Cl-2] being t he most active compound in this study.