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
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.