Repich H H, Orysyk V V, Palchykovska L G, Orysyk S I, Zborovskii Yu L, Vasylchenko O V, Storozhuk O V, Biluk A A, Nikulina V V, Garmanchuk L V, Pekhnyo V I, Vovk M V
V.I. Vernadskii Institute of General and Inorganic Chemistry NAS of Ukraine, Palladin Ave. 32/34, 03680 Kyiv, Ukraine.
Institute of Organic Chemistry NAS of Ukraine, Murmanska Str. 5, 02660 Kyiv, Ukraine.
J Inorg Biochem. 2017 Mar;168:98-106. doi: 10.1016/j.jinorgbio.2016.12.004. Epub 2016 Dec 10.
Four novel Pd and Pt mononuclear π-coordination compounds with general formula [M(HL)Cl], M=Pd, Pt have been synthesized by reaction of [PdCl], [PtCl] anions with N-allyl-4-morpholinethiocarboxamide (HL) and N-Allyl-N'-tert-butylthiourea (HL). All complexes have been characterized by single-crystal X-ray diffraction study and H, C 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 IC indexes in range of 2·10-1.5·10М (IC of cisplatin is 5.7∙10М) 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.
通过[PdCl]、[PtCl]阴离子与N-烯丙基-4-吗啉硫代甲酰胺（HL）和N-烯丙基-N'-叔丁基硫脲（HL）反应，合成了四种通式为[M(HL)Cl]（M = Pd、Pt）的新型钯和铂单核π配位化合物。所有配合物均通过单晶X射线衍射研究和氢、碳核磁共振光谱进行了表征。在体外对HeLa细胞系测定了化合物的细胞毒性、细胞生长抑制和促凋亡活性，并与作为标准药物的顺铂进行了比较。所有复合化合物均具有显著的细胞毒性活性，IC指数范围为2·10 - 1.5·10М（顺铂的IC为5.7∙10М），并且显示出比顺铂更高或相当的促凋亡、细胞生长抑制和抗合成作用。通过琼脂糖凝胶电泳监测顺铂和合成的金属配合物对pTZ19R*质粒DNA的比较影响。所有化合物均显示出对DNA的高亲和力，这与观察到的细胞生长抑制和促凋亡水平相关。总体而言，钯（II）化合物显示出比铂（II）化合物更高的活性。
