Abstract:
Substituted pyrazolo[1,5‐a]pyrimidine ligands were synthesized by cyclization, using 3‐(thiophen‐2‐yl)‐1H‐pyrazol‐5‐amine with substituted enones (3‐phenyl‐ 1‐(pyridin‐2‐yl)prop‐2‐en‐1‐one) in presence ofKOHandDMFas solvent to form
cyclic aromatic compounds. The substituted pyrazolo[1,5‐a] pyrimidine based
binuclear PtII complexes containing neutral tetradentated ligands have general
formula [Pt2(5a–5f)Cl4], (where, (5a ‐5f) = pyrazolo[1,5‐a] pyrimidine ligand).
This compounds were characterized by physicochemical and spectroscopic
method like elemental analyses, UV‐Visible, FT‐IR, EDX, TGA, molar conductivity,
magnetic susceptibility measurements, mass spectroscopy, 1H and 13C
NMR method. The square planar geometry was predicted by electronic spectral
study. All PtII compounds were evaluated by antimicrobial assay, in vitro brine
shrimp assay, in vivo cellular level bioassay using S. Pombe cells and anti‐tuberculosis
study. LC50 (50% lethal concentration) values of compounds are observed
between 6.450 ‐ 102.07 μg/mL. UV‐vis absorption titration, competitive displacement
assay, molecular docking and viscosity measurement were carried out to
examine the binding type and binding strength of complexes. The binding studies
suggest partial intercalative binding mode of the complexes and the observed
binding constant (Kb) values are found in the order of 6d >6b > 6c> 6a> 6e> 6 f.
The anti‐proliferative cytotoxicity of the synthesized PtII complexes (6a‐6f) were
tested against the HCT‐116 (Human Colorectal Carcinoma) cancer cell line
