Synthesis, characterization and biological activities of imidazo[1,2-a]pyridine based gold(III) metal complexes

Abstract

Five imidazo [1,2- a ]pyridine derivatives and their Au(III) complexes were synthesized. The compounds were characterized by 1 H-NMR, 13 C-NMR, IR, mass, UV-visible, elemental analysis, conductivity and magnetic measurement studies. All the compounds were screened for diverse biological activities to check the effect of coordination of Au(III) with imidazo [1,2- a ]pyridine heterocycles. The DNA interaction ability of compounds were studied as the change in absorption maxima and position of HS-DNA in presence of compounds and viscosity measurement due to change in DNA length under the influence of compounds. The computational insight of compound-DNA interaction was taken in docking study. All the results suggest intercalation mode of binding. The cellular level cytotoxic nature of compounds was evaluated using trypan blue dye staining of dead cell in cell viability assay. The smearing of DNA was observed, while DNA extracted from S. pombe cells in presence of complexes was subjected to gel electrophoresis, which shows their toxic effect on DNA. The complexes were evaluated for cytotoxicity on human A549 (Lung adenocarcinoma) cell line by MTT assay (IC 50 values). The in vitro cytotoxicity in terms of LC 50 value was checked on a simple zoological organism, brine shrimp.

DNA interaction, cytotoxicity and molecular structure of cobalt complex of 4‐amino‐N‐(6‐chloropyridazin‐3‐yl)benzene sulfonamide in the presence of secondary ligand pyridine

“…[35] The result shows the effects of the compound on the integrity of DNA. [35] The result shows the effects of the compound on the integrity of DNA.…”

“…(%)/found (%): C, 35 Anhydrous yield (Co-SCP) dissolve in pyridine solvent, kept into crystallizations at 293 K. Over long period of time reddish well-shaped single crystals of the compounds are found (Scheme 1).…”

“…Also in vivo cytotoxicity of complex was checked on S. pombe cells according to the literature procedure. [35]…”

Spectroscopic and electrochemical study for evaluating DNA interaction activity of 4‐(3‐halophenyl)‐6‐(pyridin‐2‐yl)pyrimidin‐2‐amine based piano stool Cp* Rh (III) and Ir (III) complexes

“…However, FDA approved Pt drugs includes only three name (cisplatin, oxaliplatin and carboplatin for cancer chemotherapy, due to inappropriate distribution in cell and inactivation by some cellular mechanism . These open up a great scope for researchers of medicinal inorganic chemistry to design and synthesize metallonuclease agents, which can specifically interact with the tumor cell and damage cellular DNA damage by forming metal‐DNA adduct, and a wide range of transition‐metal based biologically active compounds are currently under consideration for future development …”

“…[2] However, FDA approved Pt drugs includes only three name (cisplatin, oxaliplatin and carboplatin for cancer chemotherapy, due to inappropriate distribution in cell and inactivation by some cellular mechanism. [3] These open up a great scope for researchers of medicinal inorganic chemistry to design and synthesize metallonuclease agents, [4,5] which can specifically interact with the tumor cell and damage cellular DNA damage by forming metal-DNA adduct, [6] and a wide range of transition-metal based biologically active compounds are currently under consideration for future development. [7][8][9][10][11][12] In this context, half sandwich organometallic complexes with biological active ligands [13] have been extensively researched for evaluation of their anticancer activities with some of the complexes being clinical evaluated having good cytotoxicity than cisplatin.…”