Identification of β-hematin inhibitors in the MMV Malaria Box

Autor: Kim Y. Fong, Rebecca D. Sandlin, David W. Wright

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance, Vol 5, Iss 3, Pp 84-91 (2015)

The Malaria Box, assembled by the Medicines for Malaria Venture, is a set of 400 structurally diverse, commercially available compounds with demonstrated activity against blood-stage Plasmodium falciparum. The compounds are a representative subset of

Externí odkaz: https://doaj.org/article/82b28aad5c4b4cce9d0e4e34f22cc011

Exploring the scope of new arylamino alcohol derivatives: Synthesis, antimalarial evaluation, toxicological studies, and target exploration

Autor: Giovanny Garavito, Ben M. Dunn, Silvia Galiano, David W. Wright, Miguel Quiliano, Eric Deharo, Adriana Pabón, Nathan E. Goldfarb, Adela López de Cerain, Ignacio Aldana, Adela Mendoza, Isabelle Fabing, Kim Y. Fong, Ariane Vettorazzi, Silvia Pérez-Silanes

Publikováno v: International journal for parasitology. Drugs and drug resistance
International journal for parasitology. Drugs and drug resistance, Elsevier, 2016, 6 (3), pp.184-198. ⟨10.1016/j.ijpddr.2016.09.004⟩
International Journal for Parasitology: Drugs and Drug Resistance, Vol 6, Iss 3, Pp 184-198 (2016)
Dadun. Depósito Académico Digital de la Universidad de Navarra
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International journal for parasitology. Drugs and drug resistance, 2016, 6 (3), pp.184-198. ⟨10.1016/j.ijpddr.2016.09.004⟩
International Journal for Parasitology: Drugs and Drug Resistance

Synthesis of new 1-aryl-3-substituted propanol derivatives followed by structure-activity relationship, in silico drug-likeness, cytotoxicity, genotoxicity, in silico metabolism, in silico pharmacophore modeling, and in vivo studies led to the identi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fff4cd359ed61632808953a969615398
https://doi.org/10.1016/j.ijpddr.2016.09.004

Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives : synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery

Autor: Diego A. Nieto-Aco, Xavier Fernàndez-Busquets, Isabelle Fabing, Eric Deharo, Leonardo Bonilla-Ramirez, Ariane Vettorazzi, Giovanny Garavito, Juan C. Pizarro, Adriana Pabón, Kim Y. Fong, Ernest Moles, David W. Wright, Miguel Quiliano, Ignacio Aldana, Silvia Galiano, Adela López de Cerain

Publikováno v: European Journal of Medicinal Chemistry
European Journal of Medicinal Chemistry, Elsevier, 2018, 152, pp.489-514. ⟨10.1016/j.ejmech.2018.04.038⟩
European Journal of Medicinal Chemistry, 2018, 152, pp.489-514. ⟨10.1016/j.ejmech.2018.04.038⟩

International audience; Design, synthesis, structure-activity relationship, cytotoxicity studies, in silico drug-likeness, genotoxicity screening, and in vivo studies of new 1-aryl-3-substituted propanol derivatives led to the identification of nine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b37182ea0f6ad3d78da99b8184fac0ff
http://www.documentation.ird.fr/hor/fdi:010073135

Identification of β-hematin inhibitors in a high-throughput screening effort reveals scaffolds with in vitro antimalarial activity

Autor: Timothy J. Egan, Kim Y. Fong, Rebecca D. Sandlin, Kathryn J. Wicht, Holly M. Carrell, David W. Wright

Publikováno v: International Journal for Parasitology: Drugs and Drug Resistance, Vol 4, Iss 3, Pp 316-325 (2014)
International Journal for Parasitology: Drugs and Drug Resistance

Graphical abstract
Highlights • Hemozoin formation is a prime drug target pathway to probe for new lead compounds. • We examined the VICB library of compounds for in vitro β-hematin inhibition. • β-Hematin inhibitors were tested for in v

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd1286fecd3bbd60ae71b7d5c33c19bb
http://www.sciencedirect.com/science/article/pii/S2211320714000220

Hemozoin and antimalarial drug discovery

Autor: David W. Wright, Kim Y. Fong

Recent initiatives to develop more effective and affordable drugs, controlling mosquitoes and development of a preventative vaccine have been launched with the goal of completely eradicating malaria. To this end, Novartis (Surrey, UK) and GlaxoSmithK

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc3f1a447d2d611199a5a442fd9d6f46
https://europepmc.org/articles/PMC4928194/