title: Cytotoxicity and antitumor activity of platinum (II) complexes of aromatic and cycloalkanecarboxylic acid hydrazides.
abstract: New platinum (II) complexes of cyclohexanecarboxylic acid hydrazide (chcah) were synthesized and characterized by elemental analysis, IR, and 1H NMR spectra. Their inhibitory effects on cell growth and macromolecular synthesis of Friend leukemia cells in culture as well as the in vivo antitumor activity towards L1210 leukemia in mice were compared with those of complexes containing differently substituted aromatic acid hydrazides. Some of the complexes exhibited antineoplastic activity. No correlation between the in vivo cytotoxicity and the in vivo antitumor activity was found. However, there was a relationship between the in vitro macromolecular synthesis inhibition profile and the in vivo antineoplastic effect, similar to that of cisplatin. On the other hand, only agents containing one amine ligand were active in vivo. The substitution of the aromatic ring by a cycloalkane residue increased significantly the antitumor effect, with [Pt(NH3)(chcah)Cl2] being the most active compound in this study.
authors.affiliation: Institute of Molecular Biology, Bulgarian Academy of Sciences, Sofia, Bulgaria.
authors.forename: D N
authors.initials: DN
authors.lastname: Kushev
authors.forename: N C
authors.initials: NC
authors.lastname: Spassovska
authors.forename: S I
authors.initials: SI
authors.lastname: Taxirov
authors.forename: K C
authors.initials: KC
authors.lastname: Grancharov
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D002455:Cell Division / Q000187:drug effects; D004273:DNA, Neoplasm / Q000096:biosynthesis; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007939:Leukemia L1210 / Q000473:pathology*; D007942:Leukemia, Experimental / Q000473:pathology*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D009363:Neoplasm Proteins / Q000096:biosynthesis; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity*; D012334:RNA, Neoplasm / Q000096:biosynthesis; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D006834:Hydrazines; D009363:Neoplasm Proteins; D009944:Organoplatinum Compounds; D012334:RNA, Neoplasm