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Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors.

As part of our ongoing endeavour to identify novel inhibitors of cancer-associated CA isoforms IX and XII as possible anticancer candidates, here we describe the design and synthesis of small library of 2-aryl-quinazolin-4-yl aminobenzoic acid derivatives (, , and ) as new non-classical CA inhibitors. On account of its significance in the anticancer drug discovery and in the development of effective CAIs, the 4-anilinoquinazoline privileged scaffold was exploited in this study. Thereafter, the free carboxylic acid functionality was appended in the (), (), or -positon () of the anilino motif to furnish the target inhibitors. All compounds were assessed for their inhibitory activities against the hCA I, II (cytosolic), IX, and XII (trans-membrane, tumour-associated) isoforms. Moreover, six quinazolines (, , and ) were chosen by the NCI-USA for anti-proliferative activity evaluation against 59 human cancer cell lines representing nine tumour subpanels.
Zainab M Elsayed, Hadia Almahli, Alessio Nocentini, Andrea Ammara, Claudiu T Supuran, Wagdy M Eldehna, Sahar M Abou-Seri

2120 related Products with: Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors.

1,000 tests0.1ml (1mg/ml) 100ul100ug100.00 ug100ug50 mg430 tests400Tests

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#36942533   2023/03/21 To Up

Efficacy and Safety of Early Administration of 4-Factor Prothrombin Complex Concentrate in Patients With Trauma at Risk of Massive Transfusion: The PROCOAG Randomized Clinical Trial.

Optimal transfusion strategies in traumatic hemorrhage are unknown. Reports suggest a beneficial effect of 4-factor prothrombin complex concentrate (4F-PCC) on blood product consumption.
Pierre Bouzat, Jonathan Charbit, Paer-Selim Abback, Delphine Huet-Garrigue, Nathalie Delhaye, Marc Leone, Guillaume Marcotte, Jean-Stéphane David, Albrice Levrat, Karim Asehnoune, Julien Pottecher, Jacques Duranteau, Elie Courvalin, Anais Adolle, Dimitri Sourd, Jean-Luc Bosson, Bruno Riou, Tobias Gauss, Jean-François Payen,

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