title: Synthesis, spectral characterization of novel Pd(II), Pt(II) π-coordination compounds based on N-allylthioureas. Cytotoxic properties and DNA binding ability.
abstract: Four novel Pd2+and Pt2+mononuclear π-coordination compounds with general formula [M(HL)1,2Cl2], M=Pd2+, Pt2+have been synthesized by reaction of [PdCl4]2-, [PtCl4]2-anions with N-allyl-4-morpholinethiocarboxamide (HL1) and N-Allyl-N'-tert-butylthiourea (HL2). All complexes have been characterized by single-crystal X-ray diffraction study and1H,13C NMR spectroscopy. Cytotoxic, cytostatic and proapoptotic activities of compounds have been determined in vitro on HeLa cell line and compared with cisplatin as etalon drug. All complex compounds possessed pronounced cytotoxic activity with IC50indexes in range of 2·10-6-1.5·10-4М (IC50of cisplatin is 5.7∙10-5М) and showed proapoptotic, cytostatic and antisyntetic influence higher or comparable with cisplatin. The comparative influence of cisplatin and synthesized metal complexes on pTZ19R* plasmid DNA was monitored by agarose gel electrophoresis. All compounds showed high affinity to DNA that correlates with observed cytostatic and proapoptotic levels. In general Pd(II) compounds showed higher activity than Pt(II) ones.
authors.affiliation: V.I. Vernadskii Institute of General and Inorganic Chemistry NAS of Ukraine, Palladin Ave. 32/34, 03680 Kyiv, Ukraine. Electronic address: glebrepich@gmail.com.
authors.forename: H H
authors.initials: HH
authors.lastname: Repich
authors.affiliation: Institute of Organic Chemistry NAS of Ukraine, Murmanska Str. 5, 02660 Kyiv, Ukraine.
authors.forename: V V
authors.initials: VV
authors.lastname: Orysyk
authors.affiliation: Institute of Molecular Biology and Genetics NAS of Ukraine, Zabolotnogo Str., 150, 03680 Kyiv, Ukraine.
authors.forename: L G
authors.initials: LG
authors.lastname: Palchykovska
authors.affiliation: V.I. Vernadskii Institute of General and Inorganic Chemistry NAS of Ukraine, Palladin Ave. 32/34, 03680 Kyiv, Ukraine.
authors.forename: S I
authors.initials: SI
authors.lastname: Orysyk
authors.affiliation: Institute of Organic Chemistry NAS of Ukraine, Murmanska Str. 5, 02660 Kyiv, Ukraine.
authors.forename: Yu L
authors.initials: YL
authors.lastname: Zborovskii
authors.affiliation: Institute of Molecular Biology and Genetics NAS of Ukraine, Zabolotnogo Str., 150, 03680 Kyiv, Ukraine.
authors.forename: O V
authors.initials: OV
authors.lastname: Vasylchenko
authors.affiliation: Institute of Molecular Biology and Genetics NAS of Ukraine, Zabolotnogo Str., 150, 03680 Kyiv, Ukraine.
authors.forename: O V
authors.initials: OV
authors.lastname: Storozhuk
authors.affiliation: Taras Shevchencko National University, Educational and Scientific Centre "Institute of Biology", Glushkov Ave. 2, 03022 Kyiv, Ukraine.
authors.forename: A A
authors.initials: AA
authors.lastname: Biluk
authors.affiliation: Taras Shevchencko National University, Educational and Scientific Centre "Institute of Biology", Glushkov Ave. 2, 03022 Kyiv, Ukraine.
authors.forename: V V
authors.initials: VV
authors.lastname: Nikulina
authors.affiliation: Taras Shevchencko National University, Educational and Scientific Centre "Institute of Biology", Glushkov Ave. 2, 03022 Kyiv, Ukraine.
authors.forename: L V
authors.initials: LV
authors.lastname: Garmanchuk
authors.affiliation: V.I. Vernadskii Institute of General and Inorganic Chemistry NAS of Ukraine, Palladin Ave. 32/34, 03680 Kyiv, Ukraine.
authors.forename: V I
authors.initials: VI
authors.lastname: Pekhnyo
authors.affiliation: Institute of Organic Chemistry NAS of Ukraine, Murmanska Str. 5, 02660 Kyiv, Ukraine.
authors.forename: M V
authors.initials: MV
authors.lastname: Vovk
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004247:DNA / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D010165:Palladium / Q000737:chemistry*; D010984:Platinum / Q000737:chemistry*; D013890:Thiourea / Q000031:analogs & derivatives* / Q000737:chemistry; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D010984:Platinum; D010165:Palladium; C009842:allylthiourea; D004247:DNA; D013890:Thiourea
keywords: Anticancer; Cytotoxicity; DNA interaction; Palladium; Platinum; Thioureas