Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: an<i>in silico</i>and<i>in vitro</i>approach
Sandhya Chahal, Jyoti Punia, Payal Rani, Rajvir Singh, Mayank Mayank, Prof Parvin Kumar, Ramesh Kataria, Gaurav Joshi, Jayant Sindhu
Abstract
values from 0.23 ± 0.003 to 0.5 ± 0.0 μM. Along with this, the proliferations of the HCT-116, A549 and MDA-MB-231 cells were inhibited when treated with the synthesized compounds. Notable cancer cell growth inhibition was observed for compounds 5e, 5f and 5y, which correlated with their α-amylase inhibition. Additionally, the kinetics investigation revealed that 5b, 5e, 5f and 5y exhibit uncompetitive inhibition. 5b was found to be the least cytotoxic and most potent α-amylase inhibitor and was further validated by absorption and fluorescence quenching technique.
Topics & Concepts
In silicoThiazoleIn vitroChemistryCombinatorial chemistryClass (philosophy)Computational biologyPharmacologyStereochemistryBiochemistryBiologyComputer scienceGeneArtificial intelligenceSynthesis and biological activityComputational Drug Discovery MethodsSynthesis and Characterization of Heterocyclic Compounds