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Research Output 1991 2019

2019

3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity

Xue, L., Shi, D. H., Harjani, J. R., Huang, F., Beveridge, J. G., Dingjan, T., Ban, K., Diab, S., Duffy, S., Lucantoni, L., Fletcher, S., Chiu, F. C. K., Blundell, S., Ellis, K., Ralph, S. A., Wirjanata, G., Teguh, S., Noviyanti, R., Chavchich, M., Creek, D. & 10 others, Price, R. N., Marfurt, J., Charman, S. A., Cuellar, M. E., Strasser, J. M., Dahlin, J. L., Walters, M. A., Edstein, M. D., Avery, V. M. & Baell, J. B., 1 Jan 2019, In : Journal of Medicinal Chemistry. 62, 5, p. 2485-2498 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A

Leaver, D. J., Cleary, B., Nguyen, N., Priebbenow, D., Lagiakos, H. R., Sanchez, J., Xue, L., Huang, F., Sun, Y., Mujumdar, P., Mudududdla, R., Varghese, S., Teguh, S., Charman, S. A., White, K. L., Katneni, K., Cuellar, M., Strasser, J. M., Dahlin, J. L., Walters, M. A. & 10 others, Street, I. P., Monahan, B. J., Jarman, K. E., Sabroux, H. J., Falk, H., Chung, M. C., Hermans, S. J., Parker, M. W., Thomas, T. & Baell, J. B., 8 Aug 2019, In : Journal of Medicinal Chemistry. 62, 15, p. 7146-7159 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Evaluation of 4-amino 2-anilinoquinazolines against Plasmodium and other apicomplexan parasites in vitro and in a P. Falciparum Humanized NOD-scid IL2R null Mouse Model of Malaria

Gilson, P. R., Nguyen, W., Poole, W. A., Teixeira, J. E., Thompson, J. K., Guo, K., Stewart, R. J., Ashton, T. D., White, K. L., Sanz, L. M., Gamo, F. J., Charman, S. A., Wittlin, S., Duffy, J., Tonkin, C. J., Tham, W. H., Crabb, B. S., Cooke, B. M., Huston, C. D., Cowman, A. F. & 1 others, Sleebs, B. E., 1 Mar 2019, In : Antimicrobial Agents and Chemotherapy. 63, 3, 15 p., e01804-18.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials

Stoye, A., Juillard, A., Tang, A. H., Legac, J., Gut, J., White, K. L., Charman, S. A., Rosenthal, P. J., Grau, G. E. R., Hunt, N. H. & Payne, R. J., 13 Jun 2019, In : Journal of Medicinal Chemistry. 62, 11, p. 5562-5578 17 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Inhibition of cytomegalovirus replication with extended-half-life synthetic ozonides

Wang, Y., Mukhopadhyay, R., Roy, S., Kapoor, A., Su, Y. P., Charman, S. A., Chen, G., Wu, J., Wang, X., Vennerstrom, J. L. & Arav-Boger, R., 1 Jan 2019, In : Antimicrobial Agents and Chemotherapy. 63, 1, 14 p., e01735-18.

Research output: Contribution to journalArticleResearchpeer-review

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions

Lee, J., Vinh, N. B., Drinkwater, N., Yang, W., Kannan Sivaraman, K., Schembri, L. S., Gazdik, M., Grin, P. M., Butler, G. S., Overall, C. M., Charman, S. A., McGowan, S. & Scammells, P. J., 8 Aug 2019, In : Journal of Medicinal Chemistry. 62, 15, p. 7185-7209 25 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Ozonide Antimalarial Activity in the Context of Artemisinin-Resistant Malaria

Giannangelo, C., Fowkes, F. J. I., Simpson, J. A., Charman, S. A. & Creek, D. J., 1 Jul 2019, In : Trends in Parasitology. 35, 7, p. 529-543 15 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

Open Access
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The Development Process for Discovery and Clinical Advancement of Modern Antimalarials

Ashton, T. D., Devine, S., Mohrle, J., Laleu, B., Burrows, J. N., Charman, S., Creek, D. & Sleebs, B. E., Aug 2019, (Accepted/In press) In : Journal of Medicinal Chemistry.

Research output: Contribution to journalArticleResearchpeer-review

2018
6 Citations (Scopus)

Assessing drug efficacy against Plasmodium falciparum liver stages in vivo

Flannery, E. L., Foquet, L., Chuenchob, V., Fishbaugher, M., Billman, Z., Navarro, M. J., Betz, W., Olsen, T. M., Lee, J., Camargo, N., Nguyen, T., Schafer, C., Sack, B. K., Wilson, E. M., Saunders, J., Bial, J., Campo, B., Charman, S. A., Murphy, S. C., Phillips, M. A. & 2 others, Kappe, S. H. & Mikolajczak, S. A., 11 Jan 2018, In : JCI Insight. 3, 1, 12 p., e92587.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Derivatives of a benzoquinone acyl hydrazone with activity against Toxoplasma gondii

Sanford, A. G., Schulze, T. T., Potluri, L. P., Watson, G. F., Darner, E. B., Zach, S. J., Hemsley, R. M., Wallick, A. I., Warner, R. C., Charman, S. A., Wang, X., Vennerstrom, J. L. & Davis, P. H., 1 Dec 2018, In : International Journal for Parasitology: Drugs and Drug Resistance. 8, 3, p. 488-492 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria"

Brunschwig, C., Lawrence, N., Taylor, D., Abay, E., Njoroge, M., Basarab, G. S., Le Manach, C., Paquet, T., Gonzàlez Cabrera, D., Nchinda, A. T., de Kock, C., Wiesner, L., Denti, P., Waterson, D., Blasco, B., Leroy, D., Witty, M. J., Donini, C., Duffy, J., Wittlin, S. & 28 others, White, K. L., Charman, S. A., Jiménez-Díaz, M. B., Angulo-Barturen, I., Herreros, E., Gamo, F. J., Rochford, R., Mancama, D., Coetzer, T. L., van der Watt, M. E., Reader, J., Birkholtz, L. M., Marsh, K. C., Solapure, S. M., Burke, J. E., McPhail, J. A., Vanaerschot, M., Fidock, D. A., Fish, P. V., Siegl, P., Smith, D. A., Wirjanata, G., Noviyanti, R., Price, R. N., Marfurt, J., Silue, K. D., Street, L. J. & Chibale, K., 1 Nov 2018, In : Antimicrobial Agents and Chemotherapy. 62, 11

Research output: Contribution to journalComment / DebateOtherpeer-review

Open Access
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19 Citations (Scopus)

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth

Baell, J. B., Leaver, D. J., Hermans, S. J., Kelly, G. L., Brennan, M. S., Downer, N. L., Nguyen, N., Wichmann, J., McRae, H. M., Yang, Y., Cleary, B., Lagiakos, H. R., Mieruszynski, S., Pacini, G., Vanyai, H. K., Bergamasco, M. I., May, R. E., Davey, B. K., Morgan, K. J., Sealey, A. J. & 32 others, Wang, B., Zamudio, N., Wilcox, S., Garnham, A. L., Sheikh, B. N., Aubrey, B. J., Doggett, K., Chung, M. C., de Silva, M., Bentley, J., Pilling, P., Hattarki, M., Dolezal, O., Dennis, M. L., Falk, H., Ren, B., Charman, S. A., White, K. L., Rautela, J., Newbold, A., Hawkins, E. D., Johnstone, R. W., Huntington, N. D., Peat, T. S., Heath, J. K., Strasser, A., Parker, M. W., Smyth, G. K., Street, I. P., Monahan, B. J., Voss, A. K. & Thomas, T., 9 Aug 2018, In : Nature. 560, 7717, p. 253-257 5 p.

Research output: Contribution to journalLetterResearchpeer-review

Open Access
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5 Citations (Scopus)

Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity

Kokkonda, S., El Mazouni, F., White, K. L., White, J., Shackleford, D. M., Lafuente-Monasterio, M. J., Manjalanagara, K., Joseph, J. T., Garcia-Pérez, A., Fernandez, J., Gamo, F. J., Waterson, D., Burrows, J. N., Palmer, M. J., Charman, S. A., Rathod, P. K. & Phillips, M. A., Aug 2018, In : ACS Omega. 3, 8, p. 9227-9240 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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3 Citations (Scopus)

Novel Toxoplasma gondii inhibitor chemotypes

Sanford, A. G., Schulze, T. T., Potluri, L. P., Hemsley, R. M., Larson, J. J., Judge, A. K., Zach, S. J., Wang, X., Charman, S. A., Vennerstrom, J. L. & Davis, P. H., 1 Apr 2018, In : Parasitology International. 67, 2, p. 107-111 5 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Parasite-mediated degradation of synthetic ozonide antimalarials impacts in vitro antimalarial activity

Giannangelo, C., Stingelin, L., Yang, T., Tilley, L., Charman, S. A. & Creek, D. J., 1 Mar 2018, In : Antimicrobial Agents and Chemotherapy. 62, 3, 14 p., e01566-17.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Progress in antischistosomal N,N′-diaryl urea SAR

Wu, J., Wang, C., Leas, D., Vargas, M., White, K. L., Shackleford, D. M., Chen, G., Sanford, A. G., Hemsley, R. M., Davis, P. H., Dong, Y., Charman, S. A., Keiser, J. & Vennerstrom, J. L., 1 Feb 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 3, p. 244-248 5 p.

Research output: Contribution to journalArticleResearchpeer-review

SAR of a new antischistosomal urea carboxylic acid

Wu, J., Wang, C., Häberli, C., White, K. L., Shackleford, D. M., Chen, G., Dong, Y., Charman, S. A., Keiser, J. & Vennerstrom, J. L., 15 Dec 2018, In : Bioorganic and Medicinal Chemistry Letters. 28, 23-24, p. 3648-3651 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria

O’ Neill, P. M., Stocks, P. A., Sabbani, S., Roberts, N. L., Amewu, R. K., Shore, E. R., Aljayyoussi, G., Angulo-Barturén, I., Belén, M., Jiménez-Díaz, Bazaga, S. F., Martínez, M. S., Campo, B., Sharma, R., Charman, S. A., Ryan, E., Chen, G., Shackleford, D. M., Davies, J., Nixon, G. L. & 2 others, Biagini, G. A. & Ward, S. A., 15 Jul 2018, In : Bioorganic and Medicinal Chemistry. 26, 11, p. 2996-3005 10 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Uct943, a next-generation Plasmodium falciparum pi4k inhibitor preclinical candidate for the treatment of malaria

Brunschwig, C., Lawrence, N., Taylor, D., Abay, E., Njoroge, M., Basarab, G. S., Le Manach, C., Paquet, T., Cabrera, D. G., Nchinda, A. T., De Kock, C., Wiesner, L., Denti, P., Waterson, D., Blasco, B., Leroy, D., Witty, M. J., Donini, C., Duffy, J., Wittlin, S. & 28 others, White, K. L., Charman, S. A., Jiménez-Díaz, M. B., Angulo-Barturen, I., Herreros, E., Gamo, F. J., Rochford, R., Mancama, D., Coetzer, T. L., Van der Watt, M. E., Reader, J., Birkholtz, L. M., Marsh, K. C., Solapure, S. M., Burke, J. E., McPhail, J. A., Vanaerschot, M., Fidock, D. A., Fish, P. V., Siegl, P., Smith, D. A., Wirjanata, G., Noviyanti, R., Price, R. N., Marfurt, J., Silue, K. D., Street, L. J. & Chibaleb, K., 1 Sep 2018, In : Antimicrobial Agents and Chemotherapy. 62, 9, 16 p., e00012-18.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds

Katneni, K., Pham, T., Saunders, J., Chen, G., Patil, R., White, K. L., Abla, N., Chiu, F. C. K., Shackleford, D. M. & Charman, S. A., 1 Nov 2018, In : Pharmaceutical Research. 35, 11, 13 p., 210.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2017
54 Citations (Scopus)

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

Paquet, T., Le Manach, C., Cabrera, D. G., Younis, Y., Henrich, P. P., Abraham, T. S., Lee, M. C. S., Basak, R., Ghidelli-Disse, S., Lafuente-Monasterio, M. J., Bantscheff, M., Ruecker, A., Blagborough, A. M., Zakutansky, S. E., Zeeman, A-M., White, K. L., Shackleford, D. M., Mannila, J., Morizzi, J., Scheurer, C. & 1 others, Charman, S. A., 26 Apr 2017, In : Science Translational Medicine. 9, 387, 14 p., eaad9735.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures

Schwertz, G., Witschel, M. C., Rottmann, M., Bonnert, R., Leartsakulpanich, U., Chitnumsub, P., Jaruwat, A., Ittarat, W., Schäfer, A., Aponte, R. A., Charman, S. A., White, K. L., Kundu, A., Sadhukhan, S., Lloyd, M., Freiberg, G. M., Srikumaran, M., Siggel, M., Zwyssig, A., Chaiyen, P. & 1 others, Diederich, F., 22 Jun 2017, In : Journal of Medicinal Chemistry. 60, 12, p. 4840-4860 21 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance

O'Neill, P. M., Amewu, R. K., Charman, S. A., Sabbani, S., Gnädig, N. F., Straimer, J., Fidock, D. A., Shore, E. R., Roberts, N. L., Wong, M. H. L., Hong, W. D., Pidathala, C., Riley, C., Murphy, B., Aljayyoussi, G., Gamo, F. J., Sanz, L., Rodrigues, J., Cortes, C. G., Herreros, E. & 2 others, Ryan, E. & Shackleford, D. M., 24 May 2017, In : Nature Communications. 8, 10 p., 15159.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol

Abla, N., Bashyam, S., Charman, S. A., Greco, B., Hewitt, P., Jiménez-Díaz, M. B., Katneni, K., Kubas, H., Picard, D., Sambandan, Y., Sanz, L., Smith, D., Wang, T., Willis, P., Wittlin, S. & Spangenberg, T., 14 Dec 2017, In : ACS Medicinal Chemistry Letters. 8, 12, p. 1304-1308 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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1 Citation (Scopus)

Medicinal Chemistry Case History: Discovery of the Dihydroorate Dehydrogenase Inhibitor DSM265 as an Antimalarial Drug Candidate

Phillips, M. A., Rathod, P. K., Rueckle, T., Matthews, D., Burrows, J. N. & Charman, S. A., 3 Jun 2017, Comprehensive Medicinal Chemistry III: Case Histories in Recent Drug Discovery. Chackalamannil, S., Rotella, D. & Ward, S. E. (eds.). 3 ed. Amsterdam The Netherlands: Elsevier, Vol. 8. p. 544-557 14 p. (Reference Module in Chemistry, Molecular Sciences and Chemical Engineering; vol. 8, no. 3).

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Otherpeer-review

6 Citations (Scopus)

Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans

Krake, S. H., Martinez, P. D. G., McLaren, J., Ryan, E., Chen, G., White, K., Charman, S. A., Campbell, S., Willis, P. & Dias, L. C., 27 Jan 2017, In : European Journal of Medicinal Chemistry. 126, p. 929-936 8 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis

Tran, A. T., Watson, E. E., Pujari, V., Conroy, T., Dowman, L. J., Giltrap, A. M., Pang, A., Wong, W. R., Linington, R. G., Mahapatra, S., Saunders, J., Charman, S. A., West, N. P., Bugg, T. D. H., Tod, J., Dowson, C. G., Roper, D. I., Crick, D. C., Britton, W. J. & Payne, R. J., 1 Mar 2017, In : Nature Communications. 8, 9 p., 14414.

Research output: Contribution to journalArticleResearchpeer-review

File
18 Citations (Scopus)

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439)

Dong, Y., Wang, X., Kamaraj, S., Bulbule, V. J., Chiu, F. C. K., Chollet, J., Dhanasekaran, M., Hein, C. D., Papastogiannidis, P., Morizzi, J., Shackleford, D. M., Barker, H., Ryan, E., Scheurer, C., Tang, Y., Zhao, Q., Zhou, L., White, K. L., Urwyler, H., Charman, W. N. & 4 others, Matile, H., Wittlin, S., Charman, S. A. & Vennerstrom, J. L., 13 Apr 2017, In : Journal of Medicinal Chemistry. 60, 7, p. 2654-2668 15 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

The novel compound PBT434 prevents iron mediated neurodegeneration and alpha-synuclein toxicity in multiple models of Parkinson’s disease

Finkelstein, D. I., Billings, J. L., Adlard, P. A., Ayton, S., Sedjahtera, A., Masters, C. L., Wilkins, S., Shackleford, D., Charman, S. A., Bal, W., Zawisza, I. A., Kurowska, E., Gundlach, A. L., Ma, S., Bush, A. I., Hare, D. J., Doble, P. A., Crawford, S. A., Gautier, E. C., Parsons, J. & 3 others, Huggins, P., Barnham, K. J. & Cherny, R. A., 28 Jun 2017, In : Acta neuropathologica communications. 5, 1, 16 p., 53.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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2016
32 Citations (Scopus)

A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with improved drug-like properties for treatment and prevention of malaria

Phillips, M. A., White, K., Kokkonda, S., Deng, X., White, J., El Mazouni, F., Marsh, K., Tomchick, D. R., Manjalanagara, K., Rudra, K. R., Wirjanata, G., Noviyanti, R., Price, R. N., Marfurt, J., Shackleford, D., Chiu, F., Campbell, M., Jimenez-Diaz, M. B., Bazaga, S. F., Angulo-Barturen, I. & 1 others, Charman, S., 9 Dec 2016, In : ACS Infectious Diseases. 2, 12, p. 945-957 13 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Comparison of the exposure time dependence of the activities of synthetic ozonide antimalarials and dihydroartemisinin against K13 wild-type and mutant Plasmodium falciparum strains

Yang, T., Xie, S. C., Cao, P., Giannangelo, C., McCaw, J., Creek, D. J., Charman, S. A., Klonis, N. & Tilley, L., 1 Aug 2016, In : Antimicrobial Agents and Chemotherapy. 60, 8, p. 4501-4510 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
36 Citations (Scopus)

Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins

Xie, S. C., Dogovski, C., Hanssen, E., Chiu, F., Yang, T., Crespo, M. P., Stafford, C., Batinovic, S., Teguh, S., Charman, S., Klonis, N. & Tilley, L., 2016, In : Journal of Cell Science. 129, 2, p. 406-416 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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15 Citations (Scopus)

Hit-to-lead optimization of a novel class of potent, broad-spectrum trypanosomacides

Russell, S., Rahmani, R., Jones, A. J., Newson, H. L., Neilde, K., Cotillo, I., Rahmani Khajouei, M., Ferrins, L., Qureishi, S., Nguyen, N., Martinez-Martinez, M. S., Weaver, D. F., Kaiser, M., Riley, J., Thomas, J., De Rycker, M., Read, K. D., Flematti, G. R., Ryan, E., Tanghe, S. & 6 others, Rodriguez, A., Charman, S. A., Kessler, A., Avery, V. M., Baell, J. B. & Piggott, M. J., 10 Nov 2016, In : Journal of Medicinal Chemistry. 59, 21, p. 9686-9720 35 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

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, A. T., Paquet, T., Gonzàlez Cabrera, D., Younis, Y., Han, Z., Bashyam, S., Zabiulla, M., Taylor, D., Lawrence, N., White, K. L., Charman, S. A., Waterson, D., Witty, M. J., Wittlin, S., Botha, M. E., Nondaba, S. H., Reader, J., Birkholtz, L. M. & Jiménez-Díaz, M. B., 10 Nov 2016, In : Journal of Medicinal Chemistry. 59, 21, p. 9890-9905 16 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage

Francisco, A. F., Jayawardhana, S., Lewis, M. D., White, K. L., Shackleford, D. M., Chen, G., Saunders, J., Osuna-Cabello, M., Read, K. D., Charman, S. A., Chatelain, E. & Kelly, J. M., 17 Oct 2016, In : Scientific Reports. 6, 11 p., 35351.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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27 Citations (Scopus)

Open source drug discovery: Highly potent antimalarial compounds derived from the tres cantos arylpyrroles

Williamson, A. E., Ylioja, P. M., Robertson, M. N., Antonova-Koch, Y., Avery, V., Baell, J., Batchu, H., Batra, S., Burrows, J. N., Bhattacharyya, S., Calderon, F., Charman, S., Clark, J., Crespo, B., Dean, M., Debbert, S. L., Delves, M. J., Dennis, A. S. M., Deroose, F., Duffy, S. & 3 others, Ryan, E., Wells, T. & White, K., 26 Oct 2016, In : ACS Central Science. 2, 10, p. 687-701 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
16 Citations (Scopus)

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

Drinkwater, N., Vinh, N. B., Mistry, S. N., Bamert, R. S., Ruggeri, C., Holleran, J. P., Loganathan, S., Paiardini, A., Charman, S. A., Powell, A. K., Avery, V. M., McGowan, S. & Scammells, P. J., 3 Mar 2016, In : European Journal of Medicinal Chemistry. 110, p. 43-64 22 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Revisiting the SAR of the antischistosomal aryl hydantoin (Ro 13-3978)

Wang, C., Zhao, Q., Vargas, M., Jones, J. O., White, K., Shackleford, D., Chen, G., Saunders, J., Ng, A., Chiu, F., Dong, Y., Charman, S., Keiser, J. & Vennerstrom, J. L., 8 Dec 2016, In : Journal of Medicinal Chemistry. 59, 23, p. 10705-10718 14 p.

Research output: Contribution to journalArticleResearchpeer-review

30 Citations (Scopus)

Tetrahydro-2-naphthyl and 2-Indanyl triazolopyrimidines targeting Plasmodium falciparum Dihydroorotate Dehydrogenase display potent and selective antimalarial activity

Kokkonda, S., Deng, X., White, K. L., Coteron, J. M., Marco, M., de las Heras, L., White, J., El Mazouni, F., Tomchick, D. R., Manjalanagara, K., Rudra, K. R., Chen, G., Morizzi, J., Ryan, E., Kaminsky, W., Leroy, D., Martínez-Martínez, M. S., Jimenez-Diaz, M. B., Bazaga, S. F., Angulo-Barturen, I. & 6 others, Waterson, D., Burrows, J. N., Matthews, D., Charman, S. A., Phillips, M. A. & Rathod, P. K., 9 Jun 2016, In : Journal of Medicinal Chemistry. 59, 11, p. 5416-5431 16 p.

Research output: Contribution to journalArticleResearchpeer-review

2015
10 Citations (Scopus)

6-arylpyrazine-2-carboxamides: a new core for Trypanosoma brucei inhibitors

Rahmani, R., Ban, K., Jones, A. J., Ferrins, L., Ganame, D., Sykes, M. L., Avery, V. M., White, K. L., Ryan, E., Kaiser, M., Charman, S. A. & Baell, J. B., 2015, In : Journal of Medicinal Chemistry. 58, 17, p. 6753-6765 13 p.

Research output: Contribution to journalArticleResearchpeer-review

110 Citations (Scopus)

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

Phillips, M. A., Lotharius, J., Marsh, K., White, J., Dayan, A., White, K. L., Njoroge, J. W., El Mazouni, F., Lao, Y., Kokkonda, S., Tomchick, D. R., Deng, X., Laird, T., Bhatia, S. N., March, S., Ng, C. L., Fidock, D. A., Wittlin, S., Lafuente-Monasterio, M., Gamo Benito, F. J. & 30 others, Sanz Alonso, L. M., Martinez, M. S., Jimenez-Diaz, M. B., Ferrer Bazaga, S., Angulo-Barturen, I., Haselden, J. N., Louttit, J., Cui, Y., Sridhar, A., Zeeman, A-M., Kocken, C., Sauerwein, R. W., Dechering, K., Avery, V. M., Duffy, S., Delves, M., Sinden, R., Ruecker, A., Wickham, K. S., Rochford, R., Gahagen, J., Iyer, L., Riccio, E., Mirsalis, J., Bathhurst, I., Rueckle, T., Ding, X., Campo, B., Leroy, D. & Charman, S. A., 2015, In : Science Translational Medicine. 7, 296, p. 1-12 12 p.

Research output: Contribution to journalArticleResearchpeer-review

157 Citations (Scopus)

A novel multiple-stage antimalarial agent that inhibits protein synthesis

Baragana, B., Hallyburton, I., Lee, M. C. S., Norcross, N. R., Grimaldi, R., Otto, T. D., Proto, W. R., Blagborough, A. M., Meister, S., Wirjanata, G., Ruecker, A., Upton, L. M., Abraham, T. S., Justino de Almeida, M., Pradhan, A., Porzelle, A., Martinez, M. S., Bolscher, J. M., Woodland, A., Norval, S. & 30 others, Zuccotto, F., Thomas, J., Simeons, F., Stojanovski, L., Osuna-Cabello, M., Brock, P. M., Churcher, T. S., Sala, K. A., Zakutansky, S. E., Jimenez-Diaz, M. B., Sanz, L. M., Riley, J., Basak, R., Campbell, M., Avery, V. M., Sauerwein, R. W., Dechering, K. J., Noviyanti, R., Campo, B., Frearson, J. A., Angulo-Barturen, I., Ferrer-Bazaga, S., Gamo, F-J., Wyatt, P. G., Leroy, D., Siegl, P., Delves, M. J., Kyle, D. E., Wittlin, S. & Charman, S. A., 2015, In : Nature. 522, 7556, p. 315-320 6 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

ELQ-300 prodrugs for enhanced delivery and single-dose cure of malaria

Miley, G. P., Pou, S., Winter, R., Nilsen, A., Li, Y., Kelly, J. X., Stickles, A. M., Mather, M. W., Forquer, I. P., Pershing, A. M., White, K., Shackleford, D., Saunders, J., Chen, G., Ting, L-M., Kim, K., Zakharov, L. N., Donini, C., Burrows, J. N., Valdya, A. B. & 2 others, Charman, S. A. & Riscoe, M. K., 2015, In : Antimicrobial Agents and Chemotherapy. 59, 9, p. 5555-5560 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties

Moraes, C. B., White, K. L., Braillard, S., Perez, C., Goo, J., Gaspar, L., Shackleford, D. M., Cordeiro-da-Silva, A., Thompson, R. C. A., Freitas-Junior, L. H., Charman, S. A. & Chatelain, E., 2015, In : Antimicrobial Agents and Chemotherapy. 59, 6, p. 3645-3647 3 p.

Research output: Contribution to journalArticleOtherpeer-review

Open Access
1 Citation (Scopus)

Erratum: (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium (Proceedings of the National Academy of Sciences of the United States of America (2014) 111 (E5455-E5462) 1 DOI: 10.1073/pnas.1414221111)

Jiménez-Díaz, M. B., Ebert, D., Salinas, Y., Pradhan, A., Lehane, A. M., Myrand-Lapierre, M-E., O'Loughlin, K. G., Shackleford, D. M., De Almeida, M. J., Carrillo, A. K., Clark, J. A., Dennis, A. S. M., Diep, J., Deng, X., Duffy, S., Endsley, A. N., Fedewa, G., Guiguemde, W. A., Gómez, M. G., Holbrook, G. & 30 others, Horst, J. A., Kim, C. C., Liu, J., Lee, M. C. S., Matheny, A., Santosmartínez, M., Miller, G., Rodríguez-Alejandre, A., Sanz, L. M., Sigal, M., Spillman, N. J., Stein, P. D., Wang, Z., Zhu, F., Waterson, D., Knapp, S., Shelat, A. A., Avery, V. M., Fidock, D. A., Gamo-Benito, F. J., Charman, S. A., Mirsalis, J. C., Ma, H., Ferrer, S. B., Kirk, K., Angulo-Barturen, I., Kyle, D. E., de Risi, J. L., Floyd, D. M. & Guy, R. K., 20 Oct 2015, In : Proceedings of the National Academy of Sciences. 112, 42, p. E5764

Research output: Contribution to journalComment / DebateOtherpeer-review

2 Citations (Scopus)

Evidence for the in vitro bioactivation of aminopyrazole derivatives: trapping reactive aminopyrazole intermediates using glutathione ethyl ester in human liver microsomes

Ryan, E., Morrow, B. J., Hemley, C. F., Pinson, J-A., Charman, S. A., Chiu, F. C. K. & Foitzik, R. C., 2015, In : Chemical Research in Toxicology. 28, 9, p. 1747-1752 6 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities

Witschel, M. C., Rottmann, M., Schwab, A., Leartsakulpanich, U., Chitnumsub, P., Seet, M., Tonazzi, S., Schwertz, G., Stelzer, F., Mietzner, T., McNamara, C., Thater, F., Freymond, C., Jaruwat, A., Pinthong, C., Riangrungroj, P., Oufir, M., Hamburger, M., Maser, P., Sanz-Alonso, L. M. & 5 others, Charman, S., Wittlin, S., Yuthavong, Y., Chaiyen, P. & Diederich, F., 2015, In : Journal of Medicinal Chemistry. 58, 7, p. 3117-3130 14 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Synthesis and antimalarial evaluation of amide and urea derivatives based on the thiaplakortone A natural product scaffold

Schwartz, B. D., Skinner-Adams, T. S., Andrews, K. T., Coster, M. J., Edstein, M. D., MacKenzie, D., Charman, S. A., Koltun, M., Blundell, S., Campbell, A., Pouwer, R. H., Quinn, R. J., Beattie, K. D., Healy, P. C. & Davis, R. A., 2015, In : Organic and Biomolecular Chemistry. 13, 5, p. 1558-1570 13 p.

Research output: Contribution to journalArticleResearchpeer-review

57 Citations (Scopus)

Transformation of poorly water-soluble drugs into lipophilic ionic liquids enhances oral drug exposure from lipid based formulations

Sahbaz, Y., Williams, H. D., Nguyen, T-H., Saunders, J. A., Ford, L., Charman, S. A., Scammells, P. J. & Porter, C. J., 2015, In : Molecular Pharmaceutics. 12, 6, p. 1980 - 1991 12 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Trioxolane-mediated delivery of mefloquine limits brain exposure in a mouse model of malaria

Lauterwasser, E. M. W., Fontaine, S. D., Li, H., Gut, J., Katneni, K., Charman, S. A., Rosenthal, P. J., Bogyo, M. & Renslo, A. R., 2015, In : ACS Medicinal Chemistry Letters. 6, 11, p. 1145-1149 5 p.

Research output: Contribution to journalArticleResearchpeer-review