Article info.

ABSTRACT

Received 29 Jul 2020
Revised 03 Nov 2020

Accepted 30 Nov 2020

Phosphoinositide 3-kinase gamma (PI3Kg) enzymes play significant roles in inflammatory cell recruitment to tumors and accordingly a lot of studies have targeted development of small molecule inhibitors against these enzymes for managing various chronic inflammatory disorders. In this study, a number of pyrazole substituted resorcinol derivatives have been synthesized in the laboratory and then were evaluated for the inhibitory potential against the gamma isozyme. Highest inhibitory potential was observed from the introduction of a non-polar phenyl or methyl benzyl substitution (66.4% and 59.5%) on the OH group of the resorcinol. Addition of relatively polar moiety resulted in decrease in the inhibitory potential and lowest inhibition was observed from 4-pyridyl methyl and 2-morpholino ethyl moieties (23.6% and 24.5% inhibition respectively). The results were encouraging due to remarkable inhibition showed by these compounds against the PI3K enzyme. Thus, the scaffold appears as interesting pharmacophore suitable for further development.

Keywords

PI3K gamma, pyrazole, resorcinol

Cited as: Bepary, S., Hyun, Y.S., Youn, I.K., De, T.Q. and Lee, G.H., 2020. Pyrazole substituted resorcinol derivatives with PI3Kg inhibitory potential. Can Tho University Journal of Science. 12(3): 85-89.