title: Dendrimers incorporating benzenesulfonamide moieties strongly inhibit carbonic anhydrase isoforms I-XIV.
abstract: As extension of our previous study herein we report a comprehensive investigation of poly(amidoamine) (PAMAM) dendrimers as modulators of the human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms I-XIV. Interestingly inhibitory activity was observed for the non-functionalized dendrimers against the hCA I, VII, IX, XII and XIV isoforms, whereas activation properties were reported only for the cytosolic abundant hCA II. Highly efficient inhibitory action against many isoforms having medicinal chemistry applications, such as hCA II, V, VII, IX, XII and XIV, was observed for the PAMAM functionalized counterparts bearing 4, 8, 16 and 32 benzenesulfonamide moieties. Possible applications of dendrimer-CA inhibitors as therapeutic/diagnostic agents are envisaged.
authors.affiliation: Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino, Firenze, Italy. fabrizio.carta@unifi.it.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Carta
authors.forename: Sameh M
authors.initials: SM
authors.lastname: Osman
authors.forename: Daniela
authors.initials: D
authors.lastname: Vullo
authors.forename: Zeid
authors.initials: Z
authors.lastname: AlOthman
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D024401:Carbonic Anhydrase I / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000378:metabolism; D050091:Dendrimers / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry*; D000096926:Benzenesulfonamides
chemical_list: D024401:Carbonic Anhydrase I; D002257:Carbonic Anhydrase Inhibitors; D002256:Carbonic Anhydrases; D050091:Dendrimers; D013449:Sulfonamides; D000096926:Benzenesulfonamides; C104700:PAMAM Starburst; C466621:carbonic anhydrase XIV