A series of coumarin-thiourea hybrids (4 a–o) has been synthesized, and the compounds have been evaluated against the tumour associated transmembrane isoform, human (h) carbonic anhydrase (CA) hCA IX and the less-explored cytosolic isoform, hCA XIII. All compounds exhibited potent inhibition of both isoforms, with KI values of <100 nM against hCA IX. Compound 4 b was the best inhibitor (KI=78.5 nM). All the compounds inhibited hCA XIII in the low-nanomolar to sub-micromolar range, with compound 4 b again showing the best inhibition (KI=76.3 nM). With compound 4 b as a lead, more-selective inhibitors of hCA IX and hCA XIII or dual hCA IX/XIII inhibitors might be developed.

Coumarin-Thiourea Hybrids Show Potent Carbonic Anhydrase IX and XIII Inhibitory Action / Thacker P.S.; Srikanth D.; Angeli A.; Singh P.; Chinchilli K.K.; Arifuddin M.; Supuran C.T.. - In: CHEMMEDCHEM. - ISSN 1860-7179. - ELETTRONICO. - 16:(2021), pp. 1252-1256. [10.1002/cmdc.202000915]

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

Angeli A.;Supuran C. T.
2021

Abstract

A series of coumarin-thiourea hybrids (4 a–o) has been synthesized, and the compounds have been evaluated against the tumour associated transmembrane isoform, human (h) carbonic anhydrase (CA) hCA IX and the less-explored cytosolic isoform, hCA XIII. All compounds exhibited potent inhibition of both isoforms, with KI values of <100 nM against hCA IX. Compound 4 b was the best inhibitor (KI=78.5 nM). All the compounds inhibited hCA XIII in the low-nanomolar to sub-micromolar range, with compound 4 b again showing the best inhibition (KI=76.3 nM). With compound 4 b as a lead, more-selective inhibitors of hCA IX and hCA XIII or dual hCA IX/XIII inhibitors might be developed.
2021
16
1252
1256
Thacker P.S.; Srikanth D.; Angeli A.; Singh P.; Chinchilli K.K.; Arifuddin M.; Supuran C.T.
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1305643
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