Efficient synthesis of aryldipyrromethanes in water and their application in the synthesis of corroles and dipyrromethenes

Autor: Taoufik Rohand, Eduard Dolusic, Thien H. Ngo, Wouter Maes, Wim Dehaen

Publikováno v: ARKIVOC, Vol 2007, Iss 10, Pp 307-324 (2007)

Externí odkaz: https://doaj.org/article/699b947fd04f47b6b38e2808b4120a4a

Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors

Autor: Esra Yildiz, Eduard Dolusic, Johan Wouters, Bouazza Es Saadi, Sara Modaffari, Julien R. C. Prevost, Lionel Pochet, Didier M. Lambert, Raphaël Frédérick, Arina Kozlova

Publikováno v: Tetrahedron Letters, Vol. 59, no.49, p. 4315-4319 (2018)

Highly functionalized 5-bromo-2-amino-1,3-thiazoles bearing various substituents could be easily prepared by a rapid and efficient one-pot method, using simple starting materials and mild conditions while avoiding the use of metal catalysts or inconv

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b5b87ec49689aaed3179f083facfb6f
https://hdl.handle.net/2078.1/209011

Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A

Autor: Eduard Dolusic, Céline Meinguet, Johan Wouters, Raphaël Frédérick, Bernard Masereel, Evelyne Delfourne, Benoît Van den Eynde, Pierre Larrieu, Arnaud Rives, Sébastien Blanc, Vincent Stroobant, Thierry Ferain, Luc Pilotte, Delphine Colette

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:47-54

Tsitsikammamines are marine alkaloids whose structure is based on the pyrroloiminoquinone scaffold. These and related compounds have attracted attention due to various interesting biological properties, including cytotoxicity, topoisomerase inhibitio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68519d171373cbd13130d37ed0bce0a6
https://doi.org/10.1016/j.bmcl.2012.11.036

Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase

Autor: Luc Pilotte, Catherine Uyttenhove, Eduard Dolusic, Vincent Stroobant, Johan Wouters, Raphaël Frédérick, Benoît Van den Eynde, Etienne De Plaen, Didier Colau, Pierre Larrieu, Bernard Masereel

Publikováno v: Pilotte, L, Larrieu, P, Stroobant, V, Colau, D, Dolušić, E, Frédérick, R, De Plaen, E, Uyttenhove, C, Wouters, J, Masereel, B & Van Den Eynde, B J 2012, ' Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase ', Proceedings of the National Academy of Sciences of the United States of America, vol. 109, no. 7, pp. 2497-2502 . https://doi.org/10.1073/pnas.1113873109

Tryptophan catabolism mediated by indoleamine 2,3-dioxygenase (IDO1) is an important mechanism of peripheral immune tolerance contributing to tumoral immune resistance, and IDO1 inhibition is an active area of drug development. Tryptophan 2,3-dioxyge

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0019d17913b6cb5074fa7c722ee46216
https://doi.org/10.1073/pnas.1113873109

Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors

Autor: Laurence Moineaux, Pierre Larrieu, Benoît Van den Eynde, Vincent Stroobant, Thierry Ferain, Eduard Dolusic, Bernard Masereel, Luc Pilotte, Jean-Marie Frère, Johan Wouters, Jenny Pouyez, Moreno Galleni, Delphine Colette, Frédéric Sapunaric, Graeme Fraser, Didier Colau, Raphaël Frédérick, Sébastien Blanc

Publikováno v: European journal of medicinal chemistry / Chimica therapeutica. 46(7):3058-3065

Indoleamine 2,3-dioxygenase (IDO) is an important new therapeutic target for the treatment of cancer. With the aim of discovering novel IDO inhibitors, a virtual screen was undertaken and led to the discovery of the keto-indole derivative 1a endowed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::928bc1de51a87d92cebb05758bab8268
https://researchportal.unamur.be/en/publications/f8521be1-3e94-480e-9c35-32f021263efc