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
Mudasir Nabi PeerzadaAmir Azam

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.

Citations

Feb 19, 2019·Expert Opinion on Drug Discovery·Anu RaniVipan Kumar
Feb 10, 2019·Scientific Reports·Maria VouraMd Imtaiyaz Hassan
Aug 5, 2020·Journal of Enzyme Inhibition and Medicinal Chemistry·Mikhail KrasavinClaudiu T Supuran
Jun 27, 2020·Scientific Reports·Saleha AnwarMd Imtaiyaz Hassan
Dec 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Chao-Fan LuSai-Yang Zhang
Jul 25, 2019·Bioorganic Chemistry·Immo SerbianRené Csuk
Aug 19, 2020·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Zahoor Ahmad ParrayAsimul Islam
May 28, 2021·Journal of Asian Natural Products Research·Wang-Yu ZhaoJi-Wen Zhang

❮ Previous
Next ❯

Related Concepts

Related Feeds

Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis

Apoptosis in Cancer

Apoptosis is an important mechanism in cancer. By evading apoptosis, tumors can continue to grow without regulation and metastasize systemically. Many therapies are evaluating the use of pro-apoptotic activation to eliminate cancer growth. Here is the latest research on apoptosis in cancer.