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Séminaire Chimie ED459

Challenging design and synthesis of inhibitors of carbonic anhydrases

Dr. Raivis Žalubovskis (Latvian Institute of Organic Synthesis, Riga, Lettonie)

publié le

Le Jeudi 28 Avril 2016 à 13h45
UM FdS, Salle de Cours SC-16.01

Carbonic anhydrases (CA) are zinc containing enzymes which catalyze reversible hydration and transport of carbon dioxide and, along with other functions, provide pH regulation in cells. Among 15 isoforms of human CA special attention is dedicated to inhibition of tumor associated CA IX and CA XII,[1] where good inhibitory activities and selectivity for series of sulfocoumarin have been recently demonstrated.[2] We have found interesting design of saccharin derivatives which was driven by protein-inhibitor crystallization experiment.[3]

Design and synthesis of derivatives of sulfocoumarin and saccharin will be discussed. Overview on CA inhibition and cytotoxicity on tumor cell lines will be presented.

References

1. V. Alterio, A. Di Fiore, K. D’Ambrosio, C.T. Supuran, G. De Simone, Chem. Rev. 2012, 112, 4421–4468.
2. K. Tars, D. Vullo, A. Kazaks, J. Leitans, A. Lends, A. Grandane, R. Zalubovskis, A. Scozzafava, C.T. Supuran, J. Med. Chem. 2013, 56, 293–300 ; A. Grandane, M. Tanc, R. Zalubovskis, C.T. Supuran, Bioorg. Med. Chem. 2014, 22, 1522–1528 ; A. Grandane, M. Tanc, R. Zalubovskis, C.T. Supuran, Bioorg. Med. Chem. Lett. 2014, 24, 1256–1260.
3. J. Ivanova, J. Leitans, M. Tanc, A. Kazaks, R. Zalubovskis, C.T. Supuran, K. Tars, Chem. Commun. 2015, 51, 7108–7111.

Contact local IBMM : Dr. Jean-Yves Winum (équipe Glycochimie)

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