A Pt(ii)–Dip complex stabilizes parallel c-myc G-quadruplex

Abstract

A new G-quadruplex (GQ) stabilizer, [Pt(Dip)2](PF6)2 (Dip: 4,7-diphenyl-1,10-phenanthroline), is prepared by the microwave irradiation method. The complex can highly stabilize G-quadruplex, but has negligible interactions with duplex DNA. Aromatic anchors on the polypyridyl ligands bestow the stabilizer with a high binding preference towards parallel GQ.

Iridium Complexes as a Roadblock for DNA Polymerase during Amplification

“…Since the discovery of cisplatin, there have been continuous and long‐lasting efforts to develop optimized metal complexes for anticancer and anti‐HIV treatments with greater efficacy and minimal side effects . Recently, significant effort has gone into the development of metal complexes without platinum, for improved reactivity and lower cancer‐cell resistance . Control over key parameters such as ligand size, planarity, acid–base properties, the delicate hydrophobic–hydrophilic balance, and metal center redox state in the complexes is important for achieving the desired biological activities .…”

“…[1][2][3][4] Recently,s ignificant effort has gone into the development of metal complexes without platinum, for improved reactivity and lower cancer-cell resistance. [5][6][7][8][9] Control overk ey parameters such as ligand size, planarity,a cid-base properties, the delicate hydrophobic-hydrophilic balance, andm etal centerr edox state in the complexes is important for achieving the desired biological activities. [10][11][12] The selectivei nhibition of housekeeping proteins and fundamental processes associated with DNA (e.g.,D NA replication, repair,a nd fragmentation) can be crucial to the discoveryo f new drugs in this regard.…”

Preparation of 6/8/11-Amino/Chloro-Oxoisoaporphine and Group-10 Metal Complexes and Evaluation of Their in Vitro and in Vivo Antitumor Activity

“…Previous studies suggested that the hTERT gene core promoter contains two E-box binding sites of c-myc promoter region, which was also related to cell apoptosis and/or senescence375260. Herein, we confirmed the expression levels of two genes (hTERT and c-myc) mRNA in Hep-G2 ells treated with complexes 1 (8  μ M), 2 (15  μ M), 3 (5  μ M), 4 (18  μ M), 5 (28  μ M), 6 (14  μ M), 7 (16  μ M), 8 (10  μ M), 10 (12  μ M), and 11 (6  μ M) for 24 h (Figs 9 and S81), respectively.…”

“…In the past decade, a large number of nickel(II)2425262728, palladium(II)2930, and platinum(II)31323334353637 complexes have been reported to inhibit telomerase activity and to stabilize G4s383940. However, the antitumor activity and toxicology profiles of these metal complexes are still not satisfactory.…”

Relevance of G-quadruplex structures to pharmacogenetics

“…The first line of ligands such as the tri-substituted acridines targeted the terminal quartet present at the top and bottom of the G4 structure (Mergny et al, 2002). Platinum-derived complexes have been shown to preferentially target the MYC G4 structure over duplex DNA (Wang et al, 2013). The fluoroquinone derivative quarfloxin was the first G4-interacting compound to reach Phase II clinical trials, with potential for the treatment of neuroendocrine tumors (Drygin et al, 2009).…”