Half-sandwich iridium^III complexes with pyrazole-substituted heterocyclic frameworks and their biological applications

Abstract

Enhancement in the biological function, i.e., DNA binding, molecular docking, antiproliferative activity and DNA cleavage, of metal complexes as compared to free ligands is observed.

Interacción de ARN con doxorrubicina: Influencia del ligando y del metal en la actividad biológica de complejos organometálicos

“…For testing by a criterion, the cytotoxicity of cisplatin was also evaluated. As depicted in Figure 8A The mechanism of action of half-sandwich Ir(III) anticancer complexes may involve both an attack on DNA [131,148] and a perturbation of the redox status of cells [134]. In order to know if DNA is the target of these compounds, and clarify the differences in the cytotoxicity, reactivity against nucleobases, nucleotides, DNA and BSA, NMR, UV-Vis spectrometry, circular dichroism (CD), viscosity and DSC experiments, were carried out.…”

“…An increasing interest in new half-sandwich Iridium complexes has been recently shown [21,129,130]. The presence of pentamethylcyclopentadienyl substituent (Cp*) in half-sandwich Iridium molecules provides stability and hydrophobicity, which improve cell uptake [131]; besides, promotes the chloride leaving by increasing the positive charge on the metal, standing for the hydrolysis or the coordination of nucleobases to the metal centre. Furthermore benzimidazole and its derivatives exhibits a wide range of pharmacological properties as antihypertensive, anti-inflammatory, antibacterial, antifungal, antiviral, antioxidant, antiulcer, antiproliferative and antitumor activity including anticancer and HIV-1 integrase inhibition [132,133].…”

Synthetic Routes to Bioactive Bipyrazole Derivatives

“…Compounds 171 underwent a subsequent conversion into the 3,4′‐bipyrazoles 172 in 75–79 % yield when heated with phenylhydrazine in ethanolic solution of potassium tertiary butoxide (Scheme 41). [92] The bipyrazoles 172 exhibited remarkable antibacterial activity cytotoxic activities…”

“…Compounds 171 underwent a subsequent conversion into the 3,4'-bipyrazoles 172 in 75-79 % yield when heated with phenylhydrazine in ethanolic solution of potassium tertiary butoxide (Scheme 41). [92] The bipyrazoles in the presence of bleaching earth clay (BEC) (pH 12.5, 10 wt %) as a basic catalyst at 70-80°C (Scheme 42). [ 93] The 3,4'-bipyrazole derivatives 176 were synthesized following the sequence outlined in Scheme 43.…”

Prediction of a Nine−Membered Aromatic Heterocyclic 1,4,7−triazacyclononatetraenyl anion and its Sandwich Complexes with Divalent Lanthanides

“…Various half sandwich transition metal complexes with heterocyclic ligands are synthesized in the past and shown to have biological applications such as anticancer and antibacterial properties Moreover, full sandwich complexes of heterocyclic ligands are also predicted in the recent past …”