title: Polyamines and α-Carbonic Anhydrases.
abstract: Natural products represent a straightforward source for molecular structures bearing a vast array of chemical features and potentially useful for biomedical purposes. Recent examples of this type include the discovery of the coumarins and the polyamine natural products as atypical chemotypes for the inhibition of the metalloenzymes carbonic anhydrases (CAs; EC 4.2.2.1). CA enzymes are established pharmacological targets for important pathologies, which, among others, include glaucoma, hypoxic tumors, and central nervous system (CNS)-affecting diseases. Moreover, they are expressed in many bacteria, fungi and helminths which are the etiological agents of the majority of infectious diseases. In this context, natural products represent the ideal source of new and selective druggable CA modulators for biomedical purposes. Herein we report the state of the art on polyamines of natural origin as well as of synthetic derivatives as inhibitors of human CAs.
authors.affiliation: Laboratorio di Chimica Bioinorganica, Università degli Studi di Firenze, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy. andrea.scozzafava@unifi.it.
authors.forename: Andrea
authors.initials: A
authors.lastname: Scozzafava
authors.affiliation: NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. claudiu.supuran@unifi.it.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
authors.affiliation: NEUROFARBA Department, University of Florence, Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. fabrizio.carta@unifi.it.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Carta
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D001688:Biological Products / Q000737:chemistry; D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000737:chemistry; D003374:Coumarins / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D011700:Putrescine / Q000737:chemistry*; D013095:Spermidine / Q000737:chemistry*; D013096:Spermine / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001688:Biological Products; D002257:Carbonic Anhydrase Inhibitors; D003374:Coumarins; D013096:Spermine; D002256:Carbonic Anhydrases; D013095:Spermidine; D011700:Putrescine
keywords: CA inhibitors; polyamines; spermine