Publications

Khandelwal A, Arez F, Alves P.M, Badolo L, Brito C, Fischli C, Fontinha D, Oeuvray C, Prudêncio M, Rottmann M, Wilkins J, Yalkinoglu Ö, Bagchus W.M, Spangenberg T. Translation of liver stage activity of M5717, a Plasmodium elongation factor 2 inhibitor: from bench to bedside. Malar J. 2022;21:151. DOI: 10.1186/s12936-022-04171-0

Knaab T.C, Held J, Burckhardt B.B, Rubiano K, Okombo J, Yeo T, Mok S, Uhlemann A.C, Lungerich B, Fischli C, Pessanha de Carvalho L, Mordmüller B, Wittlin S, Fidock D.A, Kurz T. 3-Hydroxy-propanamidines, a new class of orally active antimalarials targeting Plasmodium falciparum. J Med Chem. 2021;64(6):3035-3047. DOI: 10.1021/acs.jmedchem.0c01744

Arez F, Rebelo S.P, Fontinha D, Simao D, Martins T.R, Machado M, Fischli C, Oeuvray C, Badolo L, Carrondo M.J.T, Rottmann M, Spangenberg T, Brito C, Greco B, Prudencio M, Alves P.M. Flexible 3D cell-based platforms for the discovery and profiling of novel drugs targeting Plasmodium hepatic infection. ACS Infect Dis. 2019;5(11):1831-1842. DOI: 10.1021/acsinfecdis.9b00144

Schalkwijk J, Allman E.L, Jansen P.A.M, de Vries L.E, Verhoef J.M.J, Jackowski S, Botman P.N.M, Beuckens-Schortinghuis C.A, Koolen K.M.J, Bolscher J.M, Vos M.W, Miller K, Reeves S.A, Pett H, Trevitt G, Wittlin S, Scheurer C, Sax S, Fischli C, Angulo-Barturen I, Jimenez-Diaz M.B, Josling G, Kooij T.W.A, Bonnert R, Campo B, Blaauw R.H, Rutjes Fpjt, Sauerwein R.W, Llinas M, Hermkens P.H.H, Dechering K.J. Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in Plasmodium falciparum. Sci Transl Med. 2019;11(510):eaas9917. DOI: 10.1126/scitranslmed.aas9917

Leven M, Knaab T.C, Held J, Duffy S, Meister S, Fischli C, Meitzner D, Lehmann U, Lungerich B, Kuna K, Stahlke P, Delves M.J, Buchholz M, Winzeler E.A, Avery V.M, Mordmuller B, Wittlin S, Kurz T. 3-hydroxy-N'-arylidenepropanehydrazonamides with halo-substituted phenanthrene scaffolds cure P. berghei infected mice when administered perorally. J Med Chem. 2017;60(14):6036-6044. DOI: 10.1021/acs.jmedchem.7b00140

Boss C, Aissaoui H, Amaral N, Bauer A, Bazire S, Binkert C, Brun R, Burki C, Ciana C.L, Corminboeuf O, Delahaye S, Dollinger C, Fischli C, Fischli W, Flock A, Frantz M.C, Girault M, Grisostomi C, Friedli A, Heidmann B, Hinder C, Jacob G, Le Bihan A, Malrieu S, Mamzed S, Merot A, Meyer S, Peixoto S, Petit N, Siegrist R, Trollux J, Weller T, Wittlin S. Discovery and characterization of ACT-451840: an antimalarial drug with a novel mechanism of action. ChemMedChem. 2016;11(18):1995-2014. DOI: 10.1002/cmdc.201600298

Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering K.J, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito F.J, Gnadig N.F, Heidmann B, Jimenez-Diaz M.B, Leroy D, Martinez M.S, Meyer S, Moehrle J.J, Ng C.L, Noviyanti R, Ruecker A, Sanz L.M, Sauerwein R.W, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price R.N, Weller T, Fischli W, Fidock D.A, Clozel M, Wittlin S. Characterization of novel antimalarial compound ACT-451840: preclinical assessment of activity and dose-efficacy modeling. PLoS Med. 2016;13(10):e1002138. DOI: 10.1371/journal.pmed.1002138

Lakshminarayana S.B, Freymond C, Fischli C, Yu J, Weber S, Goh A, Yeung B.K, Ho P.C, Dartois V, Diagana T.T, Rottmann M, Blasco F. Pharmacokinetics-pharmacodynamics analysis of spiroindolone analogs and KAE609 in a murine malaria model. Antimicrob Agents Chemother. 2015;59(2):1200-1210. DOI: 10.1128/AAC.03274-14

Ciana C.L, Siegrist R, Aissaoui H, Marx L, Racine S, Meyer S, Binkert C, de Kanter R, Fischli C, Wittlin S, Boss C. Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold. Bioorg Med Chem Lett. 2013;23(3):658-662. DOI: 10.1016/j.bmcl.2012.11.118

McNamara C.W, Lee M.C, Lim C.S, Lim S.H, Roland J, Nagle A, Simon O, Yeung B.K, Chatterjee A.K, McCormack S.L, Manary M.J, Zeeman A.M, Dechering K.J, Kumar T.R, Henrich P.P, Gagaring K, Ibanez M, Kato N, Kuhen K.L, Fischli C, Rottmann M, Plouffe D.M, Bursulaya B, Meister S, Rameh L, Trappe J, Haasen D, Timmerman M, Sauerwein R.W, Suwanarusk R, Russell B, Renia L, Nosten F, Tully D.C, Kocken C.H, Glynne R.J, Bodenreider C, Fidock D.A, Diagana T.T, Winzeler E.A. Targeting Plasmodium PI(4)K to eliminate malaria. Nature. 2013;504(7479):248-253. DOI: 10.1038/nature12782

Brunner R, Aissaoui H, Boss C, Bozdech Z, Brun R, Corminboeuf O, Delahaye S, Fischli C, Heidmann B, Kaiser M, Kamber J, Meyer S, Papastogiannidis P, Siegrist R, Voss T, Welford R, Wittlin S, Binkert C. Identification of a new chemical class of antimalarials. J Infect Dis. 2012;206(5):735-743. DOI: 10.1093/infdis/jis418

Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper P.B, Fischli C, Brun R, Lakshminarayana S.B, Rottmann M, Diagana T.T, Winzeler E.A, Glynne R, Tully D.C, Chatterjee A.K. Imidazolopiperazines: lead optimization of the second-generation antimalarial agents. J Med Chem. 2012;55(9):4244-4273. DOI: 10.1021/jm300041e

Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana S.B, Wu J, Ang H.Q, Zeng P, Kang M.L, Tan W, Tan M, Ye N, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Hollenbeck T, Tuntland T, Isbell J, Fischli C, Brun R, Rottmann M, Dartois V, Keller T, Diagana T, Winzeler E, Glynne R, Tully D.C, Chatterjee A.K. Imidazolopiperazines: hit to lead optimization of new antimalarial agents. J Med Chem. 2011;54(14):5116-5130. DOI: 10.1021/jm2003359

Yeung B.K, Zou B, Rottmann M, Lakshminarayana S.B, Ang S.H, Leong S.Y, Tan J, Wong J, Keller-Maerki S, Fischli C, Goh A, Schmitt E.K, Krastel P, Francotte E, Kuhen K, Plouffe D, Henson K, Wagner T, Winzeler E.A, Petersen F, Brun R, Dartois V, Diagana T.T, Keller T.H. Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria. J Med Chem. 2010;53(14):5155-5164. DOI: 10.1021/jm100410f