Dose-fractionation studies of a Plasmodium phosphatidylinositol 4-kinase inhibitor in a humanized mouse model of malaria
Gibhard, Liezl, Njoroge, Mathew, Mulubwa, Mwila, Lawrence, Nina, Smith, Dennis, Duffy, James, Le Manach, Claire, Brunschwig, Christel, Taylor, Dale, van der Westhuyzen, Renier, Street, Leslie J, Basarab, Gregory S, Chibale, Kelly
Published in Antimicrobial agents and chemotherapy (08.10.2024)
Published in Antimicrobial agents and chemotherapy (08.10.2024)
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Potentiation of rifampin activity in a mouse model of tuberculosis by activation of host transcription factor EB
Bryk, Ruslana, Mundhra, Shashirekha, Jiang, Xiuju, Wood, Madeleine, Pfau, Daniel, Weber, Elaina, Park, Suna, Zhang, Li, Wilson, Colin, Van der Westhuyzen, Renier, Street, Leslie, Chibale, Kelly, Zimmerman, Matthew, Dartois, Véronique, Pastore, Nunzia, Ballabio, Andrea, Hawryluk, Natalie, Canan, Stacie, Khetani, Vikram, Camardo, Joseph, Nathan, Carl
Published in PLoS pathogens (01.06.2020)
Published in PLoS pathogens (01.06.2020)
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Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria
Kandepedu, Nishanth, Gonzàlez Cabrera, Diego, Eedubilli, Srinivas, Taylor, Dale, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Lawrence, Nina, Paquet, Tanya, Eyermann, Charles J, Spangenberg, Thomas, Basarab, Gregory S, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (12.07.2018)
Published in Journal of medicinal chemistry (12.07.2018)
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Pyrrolo[3,4‑c]pyridine-1,3(2H)‑diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration
van der Westhuyzen, Renier, Winks, Susan, Wilson, Colin R, Boyle, Grant A, Gessner, Richard K, Soares de Melo, Candice, Taylor, Dale, de Kock, Carmen, Njoroge, Mathew, Brunschwig, Christel, Lawrence, Nina, Rao, Srinivasa P.S, Sirgel, Frederick, van Helden, Paul, Seldon, Ronnett, Moosa, Atica, Warner, Digby F, Arista, Luca, Manjunatha, Ujjini H, Smith, Paul W, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (10.12.2015)
Published in Journal of medicinal chemistry (10.12.2015)
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Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging
van der Westhuyzen, Renier, Mabhula, Amanda, Njaria, Paul M, Müller, Rudolf, Ngumbu Muhunga, Denis, Taylor, Dale, Lawrence, Nina, Njoroge, Mathew, Brunschwig, Christel, Moosa, Atica, Singh, Vinayak, Rao, Srinivasa P.S, Manjunatha, Ujjini H, Smith, Paul W, Warner, Digby F, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (08.07.2021)
Published in Journal of medicinal chemistry (08.07.2021)
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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model
Horatscheck, André, Andrijevic, Ana, Nchinda, Aloysius T, Le Manach, Claire, Paquet, Tanya, Khonde, Lutete Peguy, Dam, Jean, Pawar, Kailash, Taylor, Dale, Lawrence, Nina, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Reader, Janette, van der Watt, Mariëtte, Wicht, Kathryn, de Sousa, Ana Carolina C, Okombo, John, Maepa, Keletso, Egan, Timothy J, Birkholtz, Lyn-Marie, Basarab, Gregory S, Wittlin, Sergio, Fish, Paul V, Street, Leslie J, Duffy, James, Chibale, Kelly
Published in Journal of medicinal chemistry (12.11.2020)
Published in Journal of medicinal chemistry (12.11.2020)
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Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria
Gibhard, Liezl, Njoroge, Mathew, Paquet, Tanya, Brunschwig, Christel, Taylor, Dale, Lawrence, Nina, Abay, Efrem, Wittlin, Sergio, Wiesner, Lubbe, Street, Leslie J, Chibale, Kelly, Basarab, Gregory S
Published in Antimicrobial agents and chemotherapy (01.12.2018)
Published in Antimicrobial agents and chemotherapy (01.12.2018)
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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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Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization
Soares de Melo, Candice, Feng, Tzu-Shean, van der Westhuyzen, Renier, Gessner, Richard K., Street, Leslie J., Morgans, Garreth L., Warner, Digby F., Moosa, Atica, Naran, Krupa, Lawrence, Nina, Boshoff, Helena I.M., Barry, Clifton E., Harris, C. John, Gordon, Richard, Chibale, Kelly
Published in Bioorganic & medicinal chemistry (15.11.2015)
Published in Bioorganic & medicinal chemistry (15.11.2015)
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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
Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains
Le Manach, Claire, Paquet, Tanya, Wicht, Kathryn, Nchinda, Aloysius T, Brunschwig, Christel, Njoroge, Mathew, Gibhard, Liezl, Taylor, Dale, Lawrence, Nina, Wittlin, Sergio, Eyermann, Charles J, Basarab, Gregory S, Duffy, James, Fish, Paul V, Street, Leslie J, Chibale, Kelly
Published in Journal of medicinal chemistry (25.10.2018)
Published in Journal of medicinal chemistry (25.10.2018)
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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
Correction to “Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model”
Horatscheck, André, Andrijevic, Ana, Nchinda, Aloysius T, Le Manach, Claire, Paquet, Tanya, Khonde, Lutete Peguy, Dam, Jean, Pawar, Kailash, Taylor, Dale, Lawrence, Nina, Brunschwig, Christel, Gibhard, Liezl, Njoroge, Mathew, Reader, Janette, van der Watt, Mariëtte, Wicht, Kathryn, de Sousa, Ana Carolina C, Okombo, John, Maepa, Keletso, Egan, Timothy J, Birkholtz, Lyn-Marie, Basarab, Gregory S, Wittlin, Sergio, Fish, Paul V, Street, Leslie J, Duffy, James, Chibale, Kelly
Published in Journal of medicinal chemistry (11.02.2021)
Published in Journal of medicinal chemistry (11.02.2021)
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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
Novel Antitubercular 6‑Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure–Activity Relationship and Target Identification Studies
Wilson, Colin R, Gessner, Richard K, Moosa, Atica, Seldon, Ronnett, Warner, Digby F, Mizrahi, Valerie, Soares de Melo, Candice, Simelane, Sandile B, Nchinda, Aloysius, Abay, Efrem, Taylor, Dale, Njoroge, Mathew, Brunschwig, Christel, Lawrence, Nina, Boshoff, Helena I. M, Barry, Clifton E, Sirgel, Frederick A, van Helden, Paul, Harris, C. John, Gordon, Richard, Ghidelli-Disse, Sonja, Pflaumer, Hannah, Boesche, Markus, Drewes, Gerard, Sanz, Olalla, Santos, Gracia, Rebollo-Lopez, Maria José, Urones, Beatriz, Selenski, Carolyn, Lafuente-Monasterio, Maria Jose, Axtman, Matthew, Lelièvre, Joël, Ballell, Lluis, Mueller, Rudolf, Street, Leslie J, Ghorpade, Sandeep R, Chibale, Kelly
Published in Journal of medicinal chemistry (28.12.2017)
Published in Journal of medicinal chemistry (28.12.2017)
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Journal Article
Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis
Martinez-Grau, Maria Angeles, Valcarcel, Isabel C. Gonzalez, Early, Julie V., Gessner, Richard Klaus, de Melo, Candice Soares, de la Nava, Eva Maria Martin, Korkegian, Aaron, Ovechkina, Yulia, Flint, Lindsay, Gravelle, Anisa, Cramer, Jeff W., Desai, Prashant V., Street, Leslie J., Odingo, Joshua, Masquelin, Thierry, Chibale, Kelly, Parish, Tanya
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Journal Article
Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials
van der Watt, Mariëtte E, Reader, Janette, Churchyard, Alisje, Nondaba, Sindisiwe H, Lauterbach, Sonja B, Niemand, Jandeli, Abayomi, Sijuade, van Biljon, Riëtte A, Connacher, Jessica I, van Wyk, Roelof D J, Le Manach, Claire, Paquet, Tanya, González Cabrera, Diego, Brunschwig, Christel, Theron, Anjo, Lozano-Arias, Sonia, Rodrigues, Janneth F I, Herreros, Esperanza, Leroy, Didier, Duffy, James, Street, Leslie J, Chibale, Kelly, Mancama, Dalu, Coetzer, Theresa L, Birkholtz, Lyn-Marie
Published in Journal of antimicrobial chemotherapy (01.05.2018)
Published in Journal of antimicrobial chemotherapy (01.05.2018)
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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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