title: Platinum complexes with 5-methyl-5(4-pyridyl)hydantoin and its 3-methyl derivatives: synthesis and cytotoxic activity - quantitative structure-activity relationships.
abstract: 3,5-Dimethyl-5-(4-pyridyl)hydantoin (L) and its platinum(II) and platinum(IV) complexes with the general formula cis-[PtL(2) X(2) ] · n H(2) O and [PtL(2) Cl(4) ], where XCl, I and n = 2-4 were synthesized. A new Pt(IV) complex with 5-methyl-5-(4-pyridyl)hydantoin (L') with the formula cis-[Pt(L')(2) Cl(2) (OH)(2) ] · 5 H(2) O was also synthesized. The novel compounds were characterized by elemental analysis, IR, (1) H-, (13) C-, (195) Pt-NMR spectra and molar conductivity. The cytotoxic effects of these complexes were examined on three human tumor cell lines by MTT-dye reduction assay. These four new Pt(II) and Pt(IV) complexes and a set of another twelve Pt(II), Pt(IV), and Pd(II) complexes previously synthesized and tested were compiled and a QSAR model was derived in order to direct the further rational synthesis.
authors.affiliation: Department of Chemistry, Faculty of Pharmacy, Medical University Sofia, Bulgaria. adrigebk@abv.bg
authors.forename: Adriana
authors.initials: A
authors.lastname: Bakalova
authors.forename: Hristo
authors.initials: H
authors.lastname: Varbanov
authors.forename: Rossen
authors.initials: R
authors.lastname: Buyukliev
authors.forename: Georgi
authors.initials: G
authors.lastname: Momekov
authors.forename: Darvin
authors.initials: D
authors.lastname: Ivanov
authors.forename: Irini
authors.initials: I
authors.lastname: Doytchinova
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D006827:Hydantoins / Q000737:chemistry*; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry*; D021281:Quantitative Structure-Activity Relationship
chemical_list: C559959:5-methyl-5(4-pyridyl)hydantoin; D000970:Antineoplastic Agents; D006827:Hydantoins; D008024:Ligands; D009944:Organoplatinum Compounds; D011725:Pyridines