C2019-20 – Gold(I) and platinum(II) with isocyanide ligand complexes: Synthesis and biological activity

Technology # 19-20 In our first project, new Pt(II) complexes were synthesized by the reaction of the precursor complexes cis, cis-[Me2Pt(Œº-SMe2)2PtMe2], and cis-[(p-tolyl)2Pt(SMe2)2], with four and two equivalents of different types of isocyanide ligands (CNR; R = a; t-butyl, b; benzyl, and c; cyclohexyl isocyanide), respectively. All complexes were characterized by FTIR and NMR spectroscopies, and the structure of one of the Pt complexes was confirmed by single-crystal X-ray determination. The evaluation of the cytotoxicity of Pt complexes against three human cancer cell lines, namely A549 (non-small cell lung cancer cell line), SKOV3 (human ovarian cancer cell line), and MCF-7 (human breast cancer cell line), revealed promising antitumor activities for two of the Pt complexes in comparison with that of the standard cisplatin. Moreover, one of the Pt complexes effectively rendered apoptosis-inducing activities to the MCF-7 cancer cell line. The electrophoresis mobility shift assays on plasmids as well as molecular docking studies on DNA structures effectively revealed the specific binding site, binding mode, and the best orientation of the complexes to DNA. In our second project, the reaction of [(Me2S)AuCl] with an equimolar amount of benzyl isocyanide (PhCH2NC) ligand led to the formation of complex [(PhCH2NC)AuCl] (1). The solid‚ state structure of 1 was determined using the Xray diffraction method. Through a salt metathesis reaction, the chloride ligand in 1 was replaced by pyrimidine‚2‚ thiolate (SpyN‚àí) to afford the complex [(PhCH2NC) Au(Œ∑1‚S‚Spy)] (2), which was characterized spectroscopically. The cytotoxic activities of 1 and 2 were evaluated against three human cancer cell lines: ovarian carcinoma (SKOV3), lung carcinoma (A549) and breast carcinoma (MCF‚7). Complex 2 showed higher cytotoxicity than cisplatin against SKOV3 and MCF‚7 cancer cell lines. It showed a strong anti‚ proliferative activity with IC50 of 7.80, 6.26 and 6.14 ŒºM, compared with that measured for cisplatin which was 7.62, 12.36 and 11.47 ŒºM, against A549, SKOV3 and MCF‚ 7 cell lines, respectively. The induction of cellular apoptosis by 2 was also studied on MCF‚ 7 cell line. Our results indicated that 2 could induce apoptosis in cancerous cells in a dose‚ dependent manner. Technology Ventures ventures@uark.edu 479-575-7243

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