PMID- 19560209 OWN - NLM STAT- MEDLINE DCOM- 20091005 LR - 20131121 IS - 1873-3344 (Electronic) IS - 0162-0134 (Linking) VI - 103 IP - 8 DP - 2009 Aug TI - Cytotoxicity of cis-platinum(II) cycloaliphatic amidine complexes: Ring size and solvent effects on the biological activity. PG - 1113-9 LID - 10.1016/j.jinorgbio.2009.05.009 [doi] AB - A series of new platinum(II) amidine derivatives of the type cis-[PtCl(2)Z-NHC(NHR)Me(2)] (R=cyclopropyl, 1; cyclopentyl, 2; cyclohexyl, 3) were prepared in high yield by addition of the corresponding cyclic aliphatic amine RNH(2) to the coordinated acetonitrile ligands in cis-[PtCl(2)(NCMe)(2)]. The solution behaviour of 1-3 has been studied in DMSO, PEG 400 (polyethylene glycol) and PEG-DME 500 (polyethylene glycol dimethylether). The amidine complexes 1-3 were evaluated for their cytotoxic properties against a panel of human tumor cell lines containing examples of cervix (HeLa), breast (MCF7), lung (A549) and colon (HCT-15) cancer. Moreover, the amidine complexes were tested for their cytotoxicity against normal human fibroblasts (HFF-1). For comparison purposes, the cytotoxicity of cisplatin was examined under the same experimental conditions. The results obtained showed that PEG and PEG-DME behave as good solvents to carry out biological assays with platinum complexes which are water-insoluble and unstable in DMSO. Complexes 2 and 3 exhibited a biological activity comparable to that of cisplatin. FAU - Marzano, Cristina AU - Marzano C AD - Department of Pharmaceutical Sciences, University of Padova, Italy. FAU - Sbovata, Silvia Mazzega AU - Sbovata SM FAU - Gandin, Valentina AU - Gandin V FAU - Michelin, Rino A AU - Michelin RA FAU - Venzo, Alfonso AU - Venzo A FAU - Bertani, Roberta AU - Bertani R FAU - Seraglia, Roberta AU - Seraglia R LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20090524 PL - United States TA - J Inorg Biochem JT - Journal of inorganic biochemistry JID - 7905788 RN - 0 (Amidines) RN - 0 (Antineoplastic Agents) RN - 0 (Heterocyclic Compounds) RN - 0 (Solutions) RN - 0 (Solvents) RN - Q20Q21Q62J (Cisplatin) SB - IM MH - Amidines/*chemistry MH - Antineoplastic Agents/chemical synthesis/chemistry/*toxicity MH - Cell Line, Tumor MH - Cisplatin/*chemical synthesis/chemistry/*toxicity MH - Heterocyclic Compounds/*chemistry MH - Humans MH - Inhibitory Concentration 50 MH - Molecular Structure MH - Solutions MH - Solvents/*chemistry EDAT- 2009/06/30 09:00 MHDA- 2009/10/06 06:00 CRDT- 2009/06/30 09:00 PHST- 2008/10/31 00:00 [received] PHST- 2009/05/05 00:00 [revised] PHST- 2009/05/06 00:00 [accepted] PHST- 2009/06/30 09:00 [entrez] PHST- 2009/06/30 09:00 [pubmed] PHST- 2009/10/06 06:00 [medline] AID - S0162-0134(09)00098-1 [pii] AID - 10.1016/j.jinorgbio.2009.05.009 [doi] PST - ppublish SO - J Inorg Biochem. 2009 Aug;103(8):1113-9. doi: 10.1016/j.jinorgbio.2009.05.009. Epub 2009 May 24.