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Page 1
Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-b]pyridines.
Eagon S, Hammill JT, Sigal M, Ahn KJ, Tryhorn JE, Koch G, Belanger B, Chaplan CA, Loop L, Kashtanova AS, Yniguez K, Lazaro H, Wilkinson SP, Rice AL, Falade MO, Takahashi R, Kim K, Cheung A, DiBernardo C, Kimball JJ, Winzeler EA, Eribez K, Mittal N, Gamo FJ, Crespo B, Churchyard A, García-Barbazán I, Baum J, Anderson MO, Laleu B, Guy RK. Eagon S, et al. Among authors: winzeler ea. J Med Chem. 2020 Oct 22;63(20):11902-11919. doi: 10.1021/acs.jmedchem.0c01152. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32945666
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.
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.
Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana SB, Wu J, Ang HQ, Zeng P, Kang ML, 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 DC, Chatterjee AK. Wu T, et al. J Med Chem. 2011 Jul 28;54(14):5116-30. doi: 10.1021/jm2003359. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21644570 Free PMC article.
Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
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 PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK. Nagle A, et al. Among authors: winzeler ea. J Med Chem. 2012 May 10;55(9):4244-73. doi: 10.1021/jm300041e. Epub 2012 Apr 23. J Med Chem. 2012. PMID: 22524250 Free PMC article.
Synthesis and biological evaluation of epidithio-, epitetrathio-, and bis-(methylthio)diketopiperazines: synthetic methodology, enantioselective total synthesis of epicoccin G, 8,8'-epi-ent-rostratin B, gliotoxin, gliotoxin G, emethallicin E, and haematocin and discovery of new antiviral and antimalarial agents.
Nicolaou KC, Lu M, Totokotsopoulos S, Heretsch P, Giguère D, Sun YP, Sarlah D, Nguyen TH, Wolf IC, Smee DF, Day CW, Bopp S, Winzeler EA. Nicolaou KC, et al. Among authors: winzeler ea. J Am Chem Soc. 2012 Oct 17;134(41):17320-32. doi: 10.1021/ja308429f. Epub 2012 Oct 4. J Am Chem Soc. 2012. PMID: 22978674 Free PMC 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 multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: winzeler ea. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Nature. 2015. PMID: 26085270 Free PMC article.
242 results