Literature DB >> 33602041

Selective inhibition of carbonic anhydrase IX and XII by coumarin and psoralen derivatives.

Rita Meleddu1, Serenella Deplano1, Elias Maccioni1, Francesco Ortuso2, Filippo Cottiglia1, Daniela Secci1, Alessia Onali1, Erica Sanna1, Andrea Angeli3, Rossella Angius4, Stefano Alcaro2, Claudiu T Supuran3, Simona Distinto1.   

Abstract

A small library of coumarin and their psoralen analogues EMAC10157a-b-d-g and EMAC10160a-b-d-g has been designed and synthesised to investigate the effect of structural modifications on their inhibition ability and selectivity profile towards carbonic anhydrase isoforms I, II, IX, and XII. None of the new compounds exhibited activity towards hCA I and II isozymes. Conversely, both coumarin and psoralen derivatives were active against tumour associated isoforms IX and XII in the low micromolar or nanomolar range of concentration. These data further corroborate our previous findings on analogous derivatives, confirming that both coumarins and psoralens are interesting scaffolds for the design of isozyme selective hCA inhibitors.

Entities:  

Keywords:  coumarin; docking; hCAi; psoralen; tumour

Mesh:

Substances:

Year:  2021        PMID: 33602041      PMCID: PMC7899656          DOI: 10.1080/14756366.2021.1887171

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN: 1475-6366            Impact factor:   5.051


  59 in total

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8.  Synthesis, computational studies and assessment of in vitro inhibitory activity of umbelliferon-based compounds against tumour-associated carbonic anhydrase isoforms IX and XII.

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  5 in total

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3.  Synthesis, Biological Evaluation, and In Silico Studies of Novel Coumarin-Based 4H,5H-pyrano[3,2-c]chromenes as Potent β-Glucuronidase and Carbonic Anhydrase Inhibitors.

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Journal:  ACS Omega       Date:  2022-08-04

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Authors:  Giulia Arrighi; Adrián Puerta; Andrea Petrini; Francisco J Hicke; Alessio Nocentini; Miguel X Fernandes; José M Padrón; Claudiu T Supuran; José G Fernández-Bolaños; Óscar López
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  5 in total

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