Coumarin-Thiourea Hybrids Show Potent Carbonic Anhydrase IX and XIII Inhibitory Action.

Coumarin-Thiourea Hybrids Show Potent Carbonic Anhydrase IX and XIII Inhibitory Action.
ChemMedChem. 2020 Dec 21;:
Authors: Arifuddin M, Thacker PS, Danaboina Srikanth DS, Angeli A, Singh P, Chinchilli KK, Supuran CT
Abstract
A series of coumarin-thiourea hybrids (4a-o) was synthesized and the synthesized compounds were subjected for evaluation against the tumor-associated transmembrane isoform, hCA IX and the comparatively lesser-explored cytosolic isoform, hCA XIII. All the compounds exhibited potent inhibition of both the isoforms. Except compounds 4d and 4e, all the compounds inhibited hCA IX with a KI value of <100 nM, with compound 4b showing the best inhibition (KI = 78.5 nM).All the compounds inhibited hCA XIII in a low nanomolar to submicromolar range, with compound 4b again showing the best inhibition (KI = 76.3 nM). Hence,by taking compound 4b as a lead, it can be developed further either as a selective inhibitor of hCA IX and hCA XIII or as a dualhCA IX/XIII inihibitor.
PMID: 33346945 [PubMed - as supplied by publisher]

Source: ChemMedChem - December 21, 2020 Category: Chemistry Authors: Arifuddin M, Thacker PS, Danaboina Srikanth DS, Angeli A, Singh P, Chinchilli KK, Supuran CT Tags: ChemMedChem Source Type: research