The trypanocidal benzoxaborole AN7973 inhibits trypanosome mRNA processing
Begolo, Daniela, Vincent, Isabel M, Giordani, Federica, Pöhner, Ina, Witty, Michael J, Rowan, Timothy G, Bengaly, Zakaria, Gillingwater, Kirsten, Freund, Yvonne, Wade, Rebecca C, Barrett, Michael P, Clayton, Christine
Published in PLoS pathogens (25.09.2018)
Published in PLoS pathogens (25.09.2018)
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3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential
Younis, Yassir, Douelle, Frederic, Feng, Tzu-Shean, Cabrera, Diego González, Manach, Claire Le, Nchinda, Aloysius T, Duffy, Sandra, White, Karen L, Shackleford, David M, Morizzi, Julia, Mannila, Janne, Katneni, Kasiram, Bhamidipati, Ravi, Zabiulla, K. Mohammed, Joseph, Jayan T, Bashyam, Sridevi, Waterson, David, Witty, Michael J, Hardick, David, Wittlin, Sergio, Avery, Vicky, Charman, Susan A, Chibale, Kelly
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Veterinary trypanocidal benzoxaboroles are peptidase-activated prodrugs
Giordani, Federica, Paape, Daniel, Vincent, Isabel M, Pountain, Andrew W, Fernández-Cortés, Fernando, Rico, Eva, Zhang, Ning, Morrison, Liam J, Freund, Yvonne, Witty, Michael J, Peter, Rosemary, Edwards, Darren Y, Wilkes, Jonathan M, van der Hooft, Justin J J, Regnault, Clément, Read, Kevin D, Horn, David, Field, Mark C, Barrett, Michael P
Published in PLoS pathogens (03.11.2020)
Published in PLoS pathogens (03.11.2020)
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Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1
Le Manach, Claire, Gonzàlez Cabrera, Diego, Douelle, Frederic, Nchinda, Aloysius T, Younis, Yassir, Taylor, Dale, Wiesner, Lubbe, White, Karen L, Ryan, Eileen, March, Corinne, Duffy, Sandra, Avery, Vicky M, Waterson, David, Witty, Michael J, Wittlin, Sergio, Charman, Susan A, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (27.03.2014)
Published in Journal of medicinal chemistry (27.03.2014)
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Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum
Le Manach, Claire, Scheurer, Christian, Sax, Sibylle, Schleiferböck, Sarah, Cabrera, Diego Gonzalez, Younis, Yassir, Paquet, Tanya, Street, Leslie, Smith, Peter, Ding, Xavier C, Waterson, David, Witty, Michael J, Leroy, Didier, Chibale, Kelly, Wittlin, Sergio
Published in Malaria journal (16.11.2013)
Published in Malaria journal (16.11.2013)
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Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase
Paquet, Tanya, Le Manach, Claire, Cabrera, Diego González, Younis, Yassir, Henrich, Philipp P, Abraham, Tara S, Lee, Marcus C S, Basak, Rajshekhar, Ghidelli-Disse, Sonja, Lafuente-Monasterio, María José, Bantscheff, Marcus, Ruecker, Andrea, Blagborough, Andrew M, Zakutansky, Sara E, Zeeman, Anne-Marie, White, Karen L, Shackleford, David M, Mannila, Janne, Morizzi, Julia, Scheurer, Christian, Angulo-Barturen, Iñigo, Martínez, María Santos, Ferrer, Santiago, Sanz, Laura María, Gamo, Francisco Javier, Reader, Janette, Botha, Mariette, Dechering, Koen J, Sauerwein, Robert W, Tungtaeng, Anchalee, Vanachayangkul, Pattaraporn, Lim, Chek Shik, Burrows, Jeremy, Witty, Michael J, Marsh, Kennan C, Bodenreider, Christophe, Rochford, Rosemary, Solapure, Suresh M, Jiménez-Díaz, María Belén, Wittlin, Sergio, Charman, Susan A, Donini, Cristina, Campo, Brice, Birkholtz, Lyn-Marie, Hanson, Kirsten K, Drewes, Gerard, Kocken, Clemens H M, Delves, Michael J, Leroy, Didier, Fidock, David A, Waterson, David, Street, Leslie J, Chibale, Kelly
Published in Science translational medicine (26.04.2017)
Published in Science translational medicine (26.04.2017)
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Identification of a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT)
Akama, Tsutomu, Zhang, Yong-Kang, Freund, Yvonne R., Berry, Pamela, Lee, Joanne, Easom, Eric E., Jacobs, Robert T., Plattner, Jacob J., Witty, Michael J., Peter, Rosemary, Rowan, Tim G., Gillingwater, Kirsten, Brun, Reto, Nare, Bakela, Mercer, Luke, Xu, Musheng, Wang, Jiangong, Liang, Hao
Published in Bioorganic & medicinal chemistry letters (01.01.2018)
Published in Bioorganic & medicinal chemistry letters (01.01.2018)
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UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria
Brunschwig, Christel, Lawrence, Nina, Taylor, Dale, Abay, Efrem, Njoroge, Mathew, Basarab, Gregory S, Le Manach, Claire, Paquet, Tanya, Cabrera, Diego Gonzàlez, Nchinda, Aloysius T, de Kock, Carmen, Wiesner, Lubbe, Denti, Paolo, Waterson, David, Blasco, Benjamin, Leroy, Didier, Witty, Michael J, Donini, Cristina, Duffy, James, Wittlin, Sergio, White, Karen L, Charman, Susan A, Jiménez-Díaz, Maria Belén, Angulo-Barturen, Iñigo, Herreros, Esperanza, Gamo, Francisco Javier, Rochford, Rosemary, Mancama, Dalu, Coetzer, Theresa L, van der Watt, Mariëtte E, Reader, Janette, Birkholtz, Lyn-Marie, Marsh, Kennan C, Solapure, Suresh M, Burke, John E, McPhail, Jacob A, Vanaerschot, Manu, Fidock, David A, Fish, Paul V, Siegl, Peter, Smith, Dennis A, Wirjanata, Grennady, Noviyanti, Rintis, Price, Ric N, Marfurt, Jutta, Silue, Kigbafori D, Street, Leslie J, Chibale, Kelly
Published in Antimicrobial agents and chemotherapy (01.09.2018)
Published in Antimicrobial agents and chemotherapy (01.09.2018)
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Repositioning of a Diaminothiazole Series Confirmed to Target the Cyclin-Dependent Kinase CRK12 for Use in the Treatment of African Animal Trypanosomiasis
Smith, Alasdair, Wall, Richard J, Patterson, Stephen, Rowan, Tim, Rico Vidal, Eva, Stojanovski, Laste, Huggett, Margaret, Hampton, Shahienaz E, Thomas, Michael G, Corpas Lopez, Victoriano, Gillingwater, Kirsten, Duke, Jeff, Napier, Grant, Peter, Rose, Vitouley, Hervé S, Harrison, Justin R, Milne, Rachel, Jeacock, Laura, Baker, Nicola, Davis, Susan H, Simeons, Frederick, Riley, Jennifer, Horn, David, Brun, Reto, Zuccotto, Fabio, Witty, Michael J, Wyllie, Susan, Read, Kevin D, Gilbert, Ian H
Published in Journal of medicinal chemistry (14.04.2022)
Published in Journal of medicinal chemistry (14.04.2022)
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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, Claire, Nchinda, Aloysius T, Paquet, Tanya, Gonzàlez Cabrera, Diego, Younis, Yassir, Han, Ze, Bashyam, Sridevi, Zabiulla, Mohammed, Taylor, Dale, Lawrence, Nina, White, Karen L, Charman, Susan A, Waterson, David, Witty, Michael J, Wittlin, Sergio, Botha, Mariëtte E, Nondaba, Sindisiswe H, Reader, Janette, Birkholtz, Lyn-Marie, Jiménez-Díaz, María Belén, Martínez, María Santos, Ferrer, Santiago, Angulo-Barturen, Iñigo, Meister, Stephan, Antonova-Koch, Yevgeniya, Winzeler, Elizabeth A, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (10.11.2016)
Published in Journal of medicinal chemistry (10.11.2016)
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Journal Article
Novel Orally Active Antimalarial Thiazoles
González Cabrera, Diego, Douelle, Frederic, Feng, Tzu-Shean, Nchinda, Aloysius T, Younis, Yassir, White, Karen L, Wu, Quoc, Ryan, Eileen, Burrows, Jeremy N, Waterson, David, Witty, Michael J, Wittlin, Sergio, Charman, Susan A, Chibale, Kelly
Published in Journal of medicinal chemistry (10.11.2011)
Published in Journal of medicinal chemistry (10.11.2011)
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Journal Article
Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2
Le Manach, Claire, Paquet, Tanya, Gonzàlez Cabrera, Diego, Younis, Yassir, Taylor, Dale, Wiesner, Lubbe, Lawrence, Nina, Schwager, Sylva, Waterson, David, Witty, Michael J, Wittlin, Sergio, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (13.11.2014)
Published in Journal of medicinal chemistry (13.11.2014)
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Journal Article
Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries
Younis, Yassir, Street, Leslie J, Waterson, David, Witty, Michael J, Chibale, Kelly
Published in Journal of medicinal chemistry (24.10.2013)
Published in Journal of medicinal chemistry (24.10.2013)
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Journal 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, Claire, Paquet, Tanya, Brunschwig, Christel, Njoroge, Mathew, Han, Ze, Gonzàlez Cabrera, Diego, Bashyam, Sridevi, Dhinakaran, Rajkumar, Taylor, Dale, Reader, Janette, Botha, Mariette, Churchyard, Alisje, Lauterbach, Sonja, Coetzer, Theresa L, Birkholtz, Lyn-Marie, Meister, Stephan, Winzeler, Elizabeth A, Waterson, David, Witty, Michael J, Wittlin, Sergio, Jiménez-Díaz, María-Belén, Santos Martínez, María, Ferrer, Santiago, Angulo-Barturen, Iñigo, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (12.11.2015)
Published in Journal of medicinal chemistry (12.11.2015)
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Journal Article
Structure–Activity-Relationship Studies around the 2‑Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity
Younis, Yassir, Douelle, Frederic, González Cabrera, Diego, Le Manach, Claire, Nchinda, Aloysius T, Paquet, Tanya, Street, Leslie J, White, Karen L, Zabiulla, K. Mohammed, Joseph, Jayan T, Bashyam, Sridevi, Waterson, David, Witty, Michael J, Wittlin, Sergio, Charman, Susan A, Chibale, Kelly
Published in Journal of medicinal chemistry (14.11.2013)
Published in Journal of medicinal chemistry (14.11.2013)
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Journal Article
Structure–Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines
Gonzàlez Cabrera, Diego, Douelle, Frederic, Le Manach, Claire, Han, Ze, Paquet, Tanya, Taylor, Dale, Njoroge, Mathew, Lawrence, Nina, Wiesner, Lubbe, Waterson, David, Witty, Michael J, Wittlin, Sergio, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (24.09.2015)
Published in Journal of medicinal chemistry (24.09.2015)
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Journal Article
Structure–Activity Relationship Studies of Orally Active Antimalarial 3,5-Substituted 2‑Aminopyridines
González Cabrera, Diego, Douelle, Frederic, Younis, Yassir, Feng, Tzu-Shean, Le Manach, Claire, Nchinda, Aloysius T, Street, Leslie J, Scheurer, Christian, Kamber, Jolanda, White, Karen L, Montagnat, Oliver D, Ryan, Eileen, Katneni, Kasiram, Zabiulla, K. Mohammed, Joseph, Jayan T, Bashyam, Sridevi, Waterson, David, Witty, Michael J, Charman, Susan A, Wittlin, Sergio, Chibale, Kelly
Published in Journal of medicinal chemistry (27.12.2012)
Published in Journal of medicinal chemistry (27.12.2012)
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Journal Article
Cell-Based Medicinal Chemistry Optimization of High Throughput Screening Hits for Orally Active Antimalarials. Part 2: Hits from SoftFocus Kinase and other Libraries: Miniperspectives Series on Phenotypic Screening for Antiinfective Targets
Younis, Yassir, Street, Leslie J, Waterson, David, Witty, Michael J, Chibale, Kelly
Published in Journal of medicinal chemistry (24.10.2013)
Published in Journal of medicinal chemistry (24.10.2013)
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Journal Article