Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box
Reader, Janette, van der Watt, Mariëtte E, Taylor, Dale, Le Manach, Claire, Mittal, Nimisha, Ottilie, Sabine, Theron, Anjo, Moyo, Phanankosi, Erlank, Erica, Nardini, Luisa, Venter, Nelius, Lauterbach, Sonja, Bezuidenhout, Belinda, Horatscheck, Andre, van Heerden, Ashleigh, Spillman, Natalie J, Cowell, Anne N, Connacher, Jessica, Opperman, Daniel, Orchard, Lindsey M, Llinás, Manuel, Istvan, Eva S, Goldberg, Daniel E, Boyle, Grant A, Calvo, David, Mancama, Dalu, Coetzer, Theresa L, Winzeler, Elizabeth A, Duffy, James, Koekemoer, Lizette L, Basarab, Gregory, Chibale, Kelly, Birkholtz, Lyn-Marié
Published in Nature communications (11.01.2021)
Published in Nature communications (11.01.2021)
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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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Journal Article
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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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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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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Journal Article
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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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 (28.08.2024)
Published in Antimicrobial agents and chemotherapy (28.08.2024)
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Journal Article
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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The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance
Murithi, James M., Deni, Ioanna, Pasaje, Charisse Flerida A., Okombo, John, Bridgford, Jessica L., Gnädig, Nina F., Edwards, Rachel L., Yeo, Tomas, Mok, Sachel, Burkhard, Anna Y., Coburn-Flynn, Olivia, Istvan, Eva S., Sakata-Kato, Tomoyo, Gomez-Lorenzo, Maria G., Cowell, Annie N., Wicht, Kathryn J., Le Manach, Claire, Kalantarov, Gavreel F., Dey, Sumanta, Duffey, Maëlle, Laleu, Benoît, Lukens, Amanda K., Ottilie, Sabine, Vanaerschot, Manu, Trakht, Ilya N., Gamo, Francisco-Javier, Wirth, Dyann F., Goldberg, Daniel E., Odom John, Audrey R., Chibale, Kelly, Winzeler, Elizabeth A., Niles, Jacquin C., Fidock, David A.
Published in Cell chemical biology (19.05.2022)
Published in Cell chemical biology (19.05.2022)
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Journal Article
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
Le Manach, Claire, Dam, Jean, Woodland, John G, Kaur, Gurminder, Khonde, Lutete P, Brunschwig, Christel, Njoroge, Mathew, Wicht, Kathryn J, Horatscheck, André, Paquet, Tanya, Boyle, Grant A, Gibhard, Liezl, Taylor, Dale, Lawrence, Nina, Yeo, Tomas, Mok, Sachel, Eastman, Richard T, Dorjsuren, Dorjbal, Talley, Daniel C, Guo, Hui, Simeonov, Anton, Reader, Janette, van der Watt, Mariëtte, Erlank, Erica, Venter, Nelius, Zawada, Jacek W, Aswat, Ayesha, Nardini, Luisa, Coetzer, Theresa L, Lauterbach, Sonja B, Bezuidenhout, Belinda C, Theron, Anjo, Mancama, Dalu, Koekemoer, Lizette L, Birkholtz, Lyn-Marie, Wittlin, Sergio, Delves, Michael, Ottilie, Sabine, Winzeler, Elizabeth A, von Geldern, Thomas W, Smith, Dennis, Fidock, David A, Street, Leslie J, Basarab, Gregory S, Duffy, James, Chibale, Kelly
Published in Journal of medicinal chemistry (25.02.2021)
Published in Journal of medicinal chemistry (25.02.2021)
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Journal Article
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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Journal Article
Identification of Fast-Acting 2,6-Disithstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2R gamma(null) Mouse Model of Malaria
Nchinda, Aloysius T., Le Manach, Claire, Paquet, Tanya, Cabrera, Diego Gonzalez, Wicht, Kathryn J., Brunschwig, Christel, Njoroge, Mathew, Abay, Efrem, Taylor, Dale, Lawrence, Nina, Wittlin, Sergio, Jimenez-Diaz, Maria-Belen, Santos Martinez, Maria, Ferrer, Santiago, Angulo-Barturen, Inigo, Jose Lafuente-Monasterio, Maria, Duffy, James, Burrows, Jeremy, Street, Leslie J., Chibale, Kelly
Published in Journal of medicinal chemistry (10.05.2018)
Published in Journal of medicinal chemistry (10.05.2018)
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Journal Article
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
Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a Soft Focus Kinase Library: Part 1
Le Manach, Claire, Cabrera, Diego Gonzalez, 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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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
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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