Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties

Silvia Serra, Laurence Moineaux, Christelle Vancraeynest, Bernard Masereel, Johan Wouters, Lionel Pochet, Raphaël Frédérick

Résultats de recherche: Contribution à un journal/une revueArticleRevue par des pairs

Résumé

With the aim to explore the interest of the thiosemicarbazide scaffold for the inhibition of the indoleamine 2,3-dioxygenase (IDO), a promising therapeutic target for anticancer immunotherapy, a series of 32 phenylthiosemicarbazide derivatives was prepared and their IDO inhibition evaluated. Our study demonstrated that among these derivatives, compound 14 characterized with a 4-cyanophenyl group on the thiosemicarbazide was the more potent IDO inhibitor in this series being endowed with an IC50 of 1.2 μM. The SAR depicted showed that substitution in the 3- and 4-position relative to the phenylthiosemicarbazide are very promising whereas substitution in the 2-position always leads to less potent or inactive derivatives. In fact the study highlighted a novel interesting scaffold for IDO inhibition for further development.

langue originaleAnglais
Pages (de - à)96-105
Nombre de pages10
journalEuropean Journal of Medicinal Chemistry
Volume82
Les DOIs
Etat de la publicationPublié - 23 juil. 2014

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