Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 28, Issue 9, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2020.115424
Keywords
Anticancer; Apoptosis; Carbonic anhydrase IX (CAIX) inhibitors; Ferulic acid
Funding
- Council of Scientific and Industrial Research [37(1665)/15/EMR-II]
- Indian Council of Medical Research [45/63/2018-PHA/BMS/OL]
- Indian Council of Medical Research (ICMR) [45/69/2014-PHA/BMS]
- King Saud University, Riyadh, Kingdom of Saudi Arabia [RSP-2019-122]
Ask authors/readers for more resources
Carbonic anhydrase IX (CAIX) is an emerging drug target for hypoxia associated cancers. To identify potent and selective inhibitors of CAIX, a small library of ferulic acid (FA) derivatives bearing triazole moiety has been designed, synthesized and evaluated against different human CA isoforms (CAII, CAVA & CAIX). Though most of the compounds showed CAIX inhibition in the micromolar range, compound 7i selectively inhibits CAIX in the nanomolar range (IC50 = 24 nM). In silico analysis revealed binding of 7i with the catalytically important amino acid residues of CAIX. Further, cell-based studies indicate that 7i inhibits the activity of CAIX, decreases the epithelial to mesenchymal transitions, induces apoptosis, inhibits cell migration and colonization potential of cancer cells. Taken together, these results emphasized the use of 7i as a prospective pharmacological lead molecule in CAIX targeted anticancer therapeutics.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available