Multitargeting Pt(IV) Derivatives of Cisplatin or Oxaliplatin Inhibit Tumor Growth in Mice without Inducing Neuropathic Pain.

Cisplatin and oxaliplatin are Pt(II) anticancer agents that are used to treat several cancers, usually in combination with other drugs. Their efficacy is diminished by dose-limiting peripheral neuropathy (PN) that affects ∼70% of patients. PN is caused by selective accumulation of the platinum drugs in the dorsal root ganglia (DRG), which overexpress transporters for cisplatin and oxaliplatin.

Cytotoxic Imidazolyl-Mesalazine Ester-Based Ru(II) Complexes Reduce Expression of Stemness Genes and Induce Differentiation of Oral Squamous Cell Carcinoma.

The aggressiveness and recurrence of cancer is linked to cancer stem cells (CSCs), but drugs targeting CSCs may not succeed in the clinic due to the lack of a distinct CSC subpopulation. Clinical Pt(II) drugs can increase stemness. We screened 15 Ru or Ir complexes with mesalazine or 3-aminobenzoate Schiff bases of the general formulas [Ru(p-cym)L], [Ru(p-cym)L], and [Ir(Cp*)L] (L = -) and found three complexes (, , and ) that are active against oral squamous cell carcinoma (OSCC) CSCs.

Effect of microchannel geometry and linker molecules on surface immobilization efficiency of proteins in microfluidic devices.

One of the key metrics in the design of biosensors is the presence of an effective capture layer. Surface-immobilized proteins (especially as a part of antibody-antigen combinations) are the most commonly used capture ligands in biosensors. The surface coverage of these proteins in flow-based biosensors are affected by both the linker chemistry used to attach them as well as the microchannel geometry.

Mesoporous carbon structure impregnated with 2D engineered zirconium: A sustainable adsorbent for the removal of dyes from the aqueous solution.

The key designing of new breeds of the adsorbents aimed to improve the physical, chemical and textural morphology along with surface functionalization, selectivity toward the contaminants, and regenerations efficiency. In this aspect, two adsorbents named wet oxidative and ultrasonicated zirconium impregnated composite, have been synthesized through two routes, i.e.

Effect of an Imidazole-Containing Schiff Base of an Aromatic Sulfonamide on the Cytotoxic Efficacy of N,N-Coordinated Half-Sandwich Ruthenium(II) -Cymene Complexes.

Sulfonamides have a broad range of therapeutic applications, which include the inhibition of various isoforms of carbonic anhydrases (CAs). Among the various CA isoforms, CA IX is overexpressed in tumors and regulates the pH of the tumor microenvironment. Herein we present five new ruthenium(II) -cymene complexes (-) of Schiff base ligands (-) of 4-(2-aminoethyl)benzenesulfonamide by varying the aldehyde to enhance the selective cytotoxicity toward cancer cells.

Hypoxia Active Platinum(IV) Prodrugs of Orotic Acid Selective to Liver Cancer Cells.

Platinum(IV) complexes of orotic acid selectively target liver cancer cells displaying enhanced activity and higher uptake in Hep G2. The comparatively higher expression of Organic Anion Transporter 2 (OAT2) in Hep G2 and decrease in toxicity in the presence of OAT2 inhibitor suggest its involvement in the uptake of the complexes. They are resistant to sequestration by the copper transporter ATP7B, unlike cisplatin and oxaliplatin.

Disruption of the Microtubule Network and Inhibition of VEGFR2 Phosphorylation by Cytotoxic ,-Coordinated Pt(II) and Ru(II) Complexes of Trimethoxy Aniline-Based Schiff Bases.

Platinum-based complexes are one of the most successful chemotherapeutic agents having a significant ground in cancer chemotherapy despite their side effects. During the past few decades, Ru(II) complexes have been emerging as efficient alternatives owing to their promising activities against platinum-resistant cancer. The pathway of action, lipophilicity, and cytotoxicity of a Pt or Ru complex may be tuned by varying the attached ligands, the coordination mode, and the leaving group.

Differences in Stability, Cytotoxicity, and Mechanism of Action of Ru(II) and Pt(II) Complexes of a Bidentate N,O Donor Ligand.

We report [Ru(L)(η--cym)Cl] ( and ) and [Pt(L)(DMSO)Cl] ( and ) complexes, where L is a chelate imine ligand derived from chloroethylamine and salicylaldehyde () or o-vanillin (). The complexes were characterized by single-crystal X-ray diffraction and other analytical techniques. The H nuclear magnetic resonance data show that both the Ru(II) and Pt(II) complexes start forming the aquated complex within an hour.

Effect of , Coordination and Ru Halide Bond in Enhancing Selective Toxicity of a Tyramine-Based Ru (-Cymene) Complex.

Ruthenium compounds are promising anticancer candidates owing to their lower side-effects and encouraging activities against resistant tumors. Half-sandwich piano-stool type Ru compounds of general formula [(L)Ru(η-arene)(X)] (L = chelating bidentate ligand, X = halide) have exhibited significant therapeutic potential against cisplatin-resistant tumor cell lines. In Ru (-cymene) based complexes, the change of the halide leaving group has led to several interesting features, viz.

Inhibition of 3D colon cancer stem cell spheroids by cytotoxic Ru-p-cymene complexes of mesalazine derivatives.

The Ru(ii) complex of an imidazole-mesalazine Schiff base is a unique example showing growth inhibition of 3D-colon cancer stem cell spheroids and bulk colon cancer cells at lower dosage than salinomycin or oxaliplatin. Unlike oxaliplatin which increases the expression of stemness genes (SOX2, KLF4, HES1 and Oct4), these complexes maintain a tight regulation.

Synthesis, Structure, Stability, and Inhibition of Tubulin Polymerization by Ru--Cymene Complexes of Trimethoxyaniline-Based Schiff Bases.

Four trimethoxy- and dimethoxyphenylamine-based Schiff base ()-bearing Ru--cymene complexes () of the chemical formula [Ru(η--cymene)(L)(Cl)] were synthesized, isolated in pure form, and structurally characterized using single-crystal X-ray diffraction and other analytical techniques. The complexes showed excellent antiproliferative activity against various forms of cancer that are difficult to cure, viz., triple negative human metastatic breast carcinoma MDA-MB-231, human pancreatic carcinoma MIA PaCa-2, and hepatocellular carcinoma Hep G2.

Cytotoxic Ru-p-cymene complexes of an anthraimidazoledione: halide dependent solution stability, reactivity and resistance to hypoxia deactivation.

RuII-(η6-p-cymene) complexes of anthraimidazoldione (PAIDH) based ligand bearing the formula [RuII(η6-p-cymene)(PAIDH)(X)]+ (where, X = Cl, Br and I) showed excellent in vitro antiproliferative activity (IC50 range 1-2 μM) against hepatocellular carcinoma (HepG2), human pancreatic carcinoma (MIA PaCa-2) and triple negative human metastatic breast adenocarcinoma (MDA-MB-231). The ESI-MS and 1H NMR data show that the complexes are stable in aqueous solution at pH 7.4 (4 mM NaCl) with less than 10% hydrolysis in 24 h.