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

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

  • Eur J Med Chem. 2018 Jul 15:155:13-23. doi: 10.1016/j.ejmech.2018.05.034.
Mudasir Nabi Peerzada 1,  Parvez Khan 2,  Kamal Ahmad 2,  Md Imtaiyaz Hassan 2,  Amir Azam 3
Affiliations

Affiliations

  • 1 Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025, New Delhi, India.
  • 2 Centre for Interdisciplinary Research in Basic Science, Jamia Nagar, 110 025, New Delhi, India.
  • 3 Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, 110 025, New Delhi, India. Electronic address: amir_sumbul@yahoo.co.in.
PMID: 29852328 DOI: 10.1016/j.ejmech.2018.05.034
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.

Keywords

Apoptosis; Carbonic anhydrase inhibition; Chalcone; Molecular docking; Tertiary sulfonamide.

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