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An in vitro toolbox to accelerate anti-malarial drug discovery and development.
Charman SA, Andreu A, Barker H, Blundell S, Campbell A, Campbell M, Chen G, Chiu FCK, Crighton E, Katneni K, Morizzi J, Patil R, Pham T, Ryan E, Saunders J, Shackleford DM, White KL, Almond L, Dickins M, Smith DA, Moehrle JJ, Burrows JN, Abla N. Charman SA, et al. Among authors: chiu fck. Malar J. 2020 Jan 2;19(1):1. doi: 10.1186/s12936-019-3075-5. Malar J. 2020. PMID: 31898492 Free PMC article.
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J, Crighton E, Chen G, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Huertas-Valentin L, Martinez-Martinez MS, Lafuente-Monasterio MJ, Chittimalla R, Shahi SP, Wittlin S, Waterson D, Burrows JN, Matthews D, Tomchick D, Rathod PK, Palmer MJ, Charman SA, Phillips MA. Kokkonda S, et al. Among authors: chiu fck. J Med Chem. 2020 May 14;63(9):4929-4956. doi: 10.1021/acs.jmedchem.0c00311. Epub 2020 Apr 16. J Med Chem. 2020. PMID: 32248693 Free PMC article.
Cytochrome P450-Mediated Metabolism and CYP Inhibition for the Synthetic Peroxide Antimalarial OZ439.
Shackleford DM, Chiu FCK, Katneni K, Blundell S, McLaren J, Wang X, Zhou L, Sriraghavan K, Alker AM, Hunziker D, Scheurer C, Zhao Q, Dong Y, Möhrle JJ, Abla N, Matile H, Wittlin S, Vennerstrom JL, Charman SA. Shackleford DM, et al. Among authors: chiu fck. ACS Infect Dis. 2021 Jul 9;7(7):1885-1893. doi: 10.1021/acsinfecdis.1c00225. Epub 2021 Jun 8. ACS Infect Dis. 2021. PMID: 34101429 Free PMC article.
Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria.
Charman SA, Arbe-Barnes S, Bathurst IC, Brun R, Campbell M, Charman WN, Chiu FC, Chollet J, Craft JC, Creek DJ, Dong Y, Matile H, Maurer M, Morizzi J, Nguyen T, Papastogiannidis P, Scheurer C, Shackleford DM, Sriraghavan K, Stingelin L, Tang Y, Urwyler H, Wang X, White KL, Wittlin S, Zhou L, Vennerstrom JL. Charman SA, et al. Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4400-5. doi: 10.1073/pnas.1015762108. Epub 2011 Feb 7. Proc Natl Acad Sci U S A. 2011. PMID: 21300861 Free PMC article.
A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.
Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh K, Tomchick DR, Manjalanagara K, Rudra KR, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Shackleford DM, Chiu FC, Campbell M, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Martinez MS, Lafuente-Monasterio M, Kaminsky W, Silue K, Zeeman AM, Kocken C, Leroy D, Blasco B, Rossignol E, Rueckle T, Matthews D, Burrows JN, Waterson D, Palmer MJ, Rathod PK, Charman SA. Phillips MA, et al. ACS Infect Dis. 2016 Dec 9;2(12):945-957. doi: 10.1021/acsinfecdis.6b00144. Epub 2016 Oct 4. ACS Infect Dis. 2016. PMID: 27641613 Free PMC article.
Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).
Wang C, Zhao Q, Vargas M, Jones JO, White KL, Shackleford DM, Chen G, Saunders J, Ng AC, Chiu FC, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wang C, et al. J Med Chem. 2016 Dec 8;59(23):10705-10718. doi: 10.1021/acs.jmedchem.6b01410. Epub 2016 Nov 28. J Med Chem. 2016. PMID: 27933964 Free PMC article.
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
Dong Y, Wang X, Kamaraj S, Bulbule VJ, Chiu FC, Chollet J, Dhanasekaran M, Hein CD, Papastogiannidis P, Morizzi J, Shackleford DM, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White KL, Urwyler H, Charman WN, Matile H, Wittlin S, Charman SA, Vennerstrom JL. Dong Y, et al. J Med Chem. 2017 Apr 13;60(7):2654-2668. doi: 10.1021/acs.jmedchem.6b01586. Epub 2017 Jan 18. J Med Chem. 2017. PMID: 28052200
Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials.
Laleu B, Akao Y, Ochida A, Duffy S, Lucantoni L, Shackleford DM, Chen G, Katneni K, Chiu FCK, White KL, Chen X, Sturm A, Dechering KJ, Crespo B, Sanz LM, Wang B, Wittlin S, Charman SA, Avery VM, Cho N, Kamaura M. Laleu B, et al. Among authors: chiu fck. J Med Chem. 2021 Sep 9;64(17):12582-12602. doi: 10.1021/acs.jmedchem.1c00441. Epub 2021 Aug 26. J Med Chem. 2021. PMID: 34437804 Free article.
41 results