Literature

Abstract

In the quest for novel effective carbonic anhydrase inhibitors, some sulfonamide derivatives of pyridyl-indole based chalcone were synthesized and screened in vitro for inhibitory activity against human carbonic anhydrase IX isoform. Among all the synthesized compounds (SC2 -SC11), only three compounds SC3, SC7 and SC10 were found to have better binding affinity as shown by molecular docking and fluorescence binding studies. Further, the enzyme inhibition assay and in vitro anti-tumor evaluation against MCF-7 and HepG-2 cell lines revealed that the compounds SC3, SC7 and SC10 inhibited the CA IX selectively, possessed predominant anti-proliferative potential and significantly induced apoptosis in cancerous cells.

DOI： 10.1016/j.ejmech.2018.05.034

Synthesis, characterization and biological evaluation of tertiary sulfonamide derivatives of pyridyl-indole based heteroaryl chalcone as potential carbonic anhydrase IX inhibitors and anticancer agents

European Journal of Medicinal Chemistry 2018.0

Novel benzoyl thioureido benzene sulfonamides as highly potent and selective inhibitors of carbonic anhydrase IX: optimization and bioactive studies

MedChemComm 2018.0

Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies

European Journal of Medicinal Chemistry 2019.0

Synthesis of a new series of quinoline/pyridine indole-3-sulfonamide hybrids as selective carbonic anhydrase IX inhibitors

Bioorganic & Medicinal Chemistry Letters 2022.0

Novel sulfonamide bearing coumarin scaffolds as selective inhibitors of tumor associated carbonic anhydrase isoforms IX and XII

Bioorganic & Medicinal Chemistry 2016.0

Synthesis of bulky-tailed sulfonamides incorporating pyrido[2,3- d ][1,2,4]triazolo[4,3- a ]pyrimidin-1(5H)-yl) moieties and evaluation of their carbonic anhydrases I, II, IV and IX inhibitory effects