Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells: three for the price of one

CT Supuran, V Alterio, A Di Fiore… - Medicinal Research …, 2018 - Wiley Online Library
Human carbonic anhydrase (CA) IX is a tumor‐associated protein, since it is scarcely
present in normal tissues, but highly overexpressed in a large number of solid tumors, where …

Carbonic anhydrase inhibitors as antitumor/antimetastatic agents: a patent review (2008–2018)

A Nocentini, CT Supuran - Expert Opinion on Therapeutic Patents, 2018 - Taylor & Francis
Introduction: Human carbonic anhydrases (CA, EC 4.2. 1.1) IX and XII are tumor-associated
proteins, being part of the molecular machinery that tumor cells build as adaptive responses …

Coumarin–triazole hybrids and their biological activities

YL Fan, X Ke, M Liu - Journal of Heterocyclic Chemistry, 2018 - Wiley Online Library
Hybridization is emerged as a promising strategy in the discovery of new drugs, especially
these with complimentary activities and multiple pharmacological targets that are the …

Nanoemulsions of sulfonamide carbonic anhydrase inhibitors strongly inhibit the growth of Trypanosoma cruzi

AB Vermelho, V da Silva Cardoso… - Journal of enzyme …, 2018 - Taylor & Francis
Sulfonamide carbonic anhydrase (CA, EC 4.2. 1.1) inhibitors targeting the α-class enzyme
from the protozoan pathogen Trypanosoma cruzi, responsible of Chagas disease, were …

Synthesis of novel 4-functionalized 1, 5-diaryl-1, 2, 3-triazoles containing benzenesulfonamide moiety as carbonic anhydrase I, II, IV and IX inhibitors

L Vats, V Sharma, A Angeli, R Kumar… - European journal of …, 2018 - Elsevier
The design, synthesis and biological evaluation of a library of 1, 2, 3-triazole carboxylates
incorporating carboxylic acid, hydroxymethyl, carboxylic acid hydrazide, carboxamide and …

Antileishmanial activity of sulphonamide nanoemulsions targeting the β-carbonic anhydrase from Leishmania species

V da Silva Cardoso, AB Vermelho… - Journal of Enzyme …, 2018 - Taylor & Francis
The β-carbonic anhydrase (CA, EC 4.2. 1.1) from Leishmania spp.(LdcCA) is effectively
inhibited by aromatic/heterocyclic sulphonamides, in the low nanomolar range, but no in …

Targeting tumor associated carbonic anhydrases IX and XII: highly isozyme selective coumarin and psoralen inhibitors

C Melis, S Distinto, G Bianco, R Meleddu… - ACS medicinal …, 2018 - ACS Publications
A small library of psoralen carboxylic acids and their corresponding benzenesulfonamide
derivatives were designed and synthesized to evaluate their activity and selectivity toward …

One‐pot, four‐component green synthesis, carbonic anhydrase II inhibition and docking studies of 5‐Arylidenerhodanines

A Mermer, N Demirbas, A Colak, EA Demir… - …, 2018 - Wiley Online Library
In the present study, a planning strategy for N‐substituted‐5‐arylidenerhodanines was
developed by the condensation between 3‐morpholinopropan‐1‐amine, aldehyde, ethyl …

Synthesis and single crystal X-ray diffraction studies of coumarin-based Zn (II) and Mn (II) complexes, involving supramolecular interactions

V Stefanou, D Matiadis, D Tsironis… - Polyhedron, 2018 - Elsevier
In this work we describe the synthesis and characterization of two supramolecular
coordination complexes, namely [Zn (Cuma) 2 (MeOH) 2] 2 and [Mn (Cuma) 2 (MeOH) 2] 3 …

A novel proteochemometrics model for predicting the inhibition of nine carbonic anhydrase isoforms based on supervised Laplacian score and k-nearest neighbour …

E Nazarshodeh, R Sheikhpour… - SAR and QSAR in …, 2018 - Taylor & Francis
Carbonic anhydrases (CAs) are essential enzymes in biological processes. Prediction of the
activity of compounds towards CA isoforms could be evaluated by computational techniques …