The art of developing potential anticancer molecules involves a reasonable selection of core moiety and tethering with biologically active pharmacophores. We report a library of rationally designed twelve triazole tethered benzimidazole molecules as novel potential inhibitors for cancer. Their synthesis followed a facile copper-catalysed cycloaddition reaction with good yields. Although in-silico molecular docking studies of the synthesized compounds with epigenetic protein viz., PRMTs showed inhibition, the compounds bearing amino acid and aryl groups exhibited excellent performance. The potential anti-cancer activity of the library of molecules are further evaluated in vitro against the selected cancer cell lines (MCF-7, DU145, PC3 and HepG2) besides methylation assays. In vitro results revealed that the compounds bearing amino acid and aryl groups exhibited better activity and particularly, 3-CF 3 -phenyl derivative (IC 50 = 4.11 μm against MCF-7) exerted prominent anticancer potency against all the tested cell lines. The observed strong anticancer potency of lead compound is supported by its strong binding nature noted in in-silico molecular docking studies.
N-Ethyl-3-cabazolecarboxaldehydethiosemicarbazone (ECCT) is proposed as a new, sensitive and selective complexing reagent for the separation and extractive spectrophotometric determination of palladium(II) at pH: 4.0 to form a yellowish orange colored 1:1 chelate complex, which is very well extracted in to n-butanol. The absorbance was measured at a maximum wavelength, 410 nm. This method obeys Beer's law in the concentration range 0.0-6.6 microg mL(-1) and the correlation coefficient of Pd(II)-ECCT complex is 0.998, which indicates an excellent linearity between the two variables with good molar absorptivity and Sandell's sensitivity, 1.647 x 10(4) l mol(-1)cm(-1), 6.49 x 10(-3) microg cm(-2), respectively. The instability constant of complex calculated from Edmond's method, 2.724 x 10(-5) was in good agreement with the value calculated from Asmus' method 2.624 x 10(-5), at room temperature. The precision and accuracy of the method is checked with calculation of relative standard deviation (n = 5), 0.839. Edmond's method was observed to be a more selective method in the presence of EDTA, oxalate and phosphate ions. The method was successfully applied for the determination of Pd(II) in water samples, synthetic mixtures and hydrogenation catalysts, employing an atomic absorption spectrometer for comparing these results.
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