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Page 1
Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.
Wang L, Bohmer MJ, Wang J, Nardella F, Calla J, Laureano De Souza M, Schindler KA, Montejo L, Mittal N, Rocamora F, Treat M, Charlton JT, Tumwebaze PK, Rosenthal PJ, Cooper RA, Chakrabarti R, Winzeler EA, Chakrabarti D, Gray NS. Wang L, et al. Among authors: winzeler ea. J Med Chem. 2024 Jan 25;67(2):1460-1480. doi: 10.1021/acs.jmedchem.3c02046. Epub 2024 Jan 12. J Med Chem. 2024. PMID: 38214254
Cell-based optimization of novel benzamides as potential antimalarial leads.
Wu T, Nagle A, Sakata T, Henson K, Borboa R, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Deng X, Gray NS, Tully DC, Chatterjee AK. Wu T, et al. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6970-4. doi: 10.1016/j.bmcl.2009.10.050. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2009. PMID: 19879133 Free PMC article.
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.
Deng X, Nagle A, Wu T, Sakata T, Henson K, Chen Z, Kuhen K, Plouffe D, Winzeler E, Adrian F, Tuntland T, Chang J, Simerson S, Howard S, Ek J, Isbell J, Tully DC, Chatterjee AK, Gray NS. Deng X, et al. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4027-31. doi: 10.1016/j.bmcl.2010.05.095. Epub 2010 Jun 2. Bioorg Med Chem Lett. 2010. PMID: 20610151 Free article.
Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages.
Hansen FK, Sumanadasa SD, Stenzel K, Duffy S, Meister S, Marek L, Schmetter R, Kuna K, Hamacher A, Mordmüller B, Kassack MU, Winzeler EA, Avery VM, Andrews KT, Kurz T. Hansen FK, et al. Among authors: winzeler ea. Eur J Med Chem. 2014 Jul 23;82:204-13. doi: 10.1016/j.ejmech.2014.05.050. Epub 2014 May 22. Eur J Med Chem. 2014. PMID: 24904967 Free PMC article.
Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stages.
Zou B, Nagle A, Chatterjee AK, Leong SY, Tan LJ, Sim WL, Mishra P, Guntapalli P, Tully DC, Lakshminarayana SB, Lim CS, Tan YC, Abas SN, Bodenreider C, Kuhen KL, Gagaring K, Borboa R, Chang J, Li C, Hollenbeck T, Tuntland T, Zeeman AM, Kocken CH, McNamara C, Kato N, Winzeler EA, Yeung BK, Diagana TT, Smith PW, Roland J. Zou B, et al. Among authors: winzeler ea. ACS Med Chem Lett. 2014 Jul 6;5(8):947-50. doi: 10.1021/ml500244m. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147620 Free PMC article.
A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.
Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K. Le Manach C, et al. Among authors: winzeler ea. J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2. J Med Chem. 2015. PMID: 26502160
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.
Norcross NR, Baragaña B, Wilson C, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Porzelle A, Grimaldi R, Wittlin S, Duffy S, Avery VM, Meister S, Sanz L, Jiménez-Díaz B, Angulo-Barturen I, Ferrer S, Martínez MS, Gamo FJ, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH. Norcross NR, et al. Among authors: winzeler ea. J Med Chem. 2016 Jul 14;59(13):6101-20. doi: 10.1021/acs.jmedchem.6b00028. Epub 2016 Jun 17. J Med Chem. 2016. PMID: 27314305 Free PMC article.
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.
Baragaña B, Norcross NR, Wilson C, Porzelle A, Hallyburton I, Grimaldi R, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Wyatt PG, Delves MJ, Meister S, Duffy S, Avery VM, Winzeler EA, Sinden RE, Wittlin S, Frearson JA, Gray DW, Fairlamb AH, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH. Baragaña B, et al. Among authors: winzeler ea. J Med Chem. 2016 Nov 10;59(21):9672-9685. doi: 10.1021/acs.jmedchem.6b00723. Epub 2016 Sep 10. J Med Chem. 2016. PMID: 27631715 Free PMC article.
Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.
Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K. Le Manach C, et al. Among authors: winzeler ea. J Med Chem. 2016 Nov 10;59(21):9890-9905. doi: 10.1021/acs.jmedchem.6b01265. Epub 2016 Oct 26. J Med Chem. 2016. PMID: 27748596
222 results