Publications
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| 2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy., Dziwornu GA, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu VS, Samanta S, Bhana AD, Korkor CM, Garnie LF, Teixeira N, Wicht KJ, Taylor D, Olckers R, Njoroge M, Gibhard L, Salomane N, Wittlin S, Mahato R, Chakraborty A, Sevilleno N, Coyle R, Lee MCS, Godoy LC, Pasaje CF, Niles JC, Reader J, van der Watt M, Birkholtz LM, Bolscher JM, de Bruijni MHC, Coulson LB, Basarab GS, Ghorpade SR, Chibale K. J Med Chem. 2024 Jun 25, PMID: 38918002 |
| Characterization of antimalarial activity of artemisinin-based hybrid drugs. Quadros HC, Herrmann L, Manaranche J, Paloque L, Borges-Silva MC, Dziwornu GA, D'Alessandro S, Chibale K, Basilico N, Benoit-Vical F, Tsogoeva SB, Moreira DRM. Antimicrob Agents Chemother. 2024 Jun 20:e0014324, PMID: 38899927 |
| hERG, Plasmodium Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole. Mambwe D, Coertzen D, Leshabane M, Mulubwa M, Njoroge M, Gibhard L, Girling G, Wicht KJ, Lee MCS, Wittlin S, Moreira DRM, Birkholtz LM, K. ACS Med Chem Lett. 2024 Mar 18;15(4):463-469, PMID: 38628794 |
| AI can help to tailor drugs for Africa - but Africans should lead the way. Turon G, Njoroge M, Mulubwa M, Duran-Frigola M, Chibale K. Nature. 2024 Apr;628(8007):265-267, PMID: 38594395 |
| Forging a Future Free from Neglected Tropical Diseases. da Silva Emery F, Chibale K. ACS Med Chem Lett. 2024 Feb 26;15(3):314-315, PMID: 38505853 |
| Tips for Getting Your Manuscript Accepted into ACS Medicinal Chemistry Letters. Woodland JG, Chibale K. ACS Med Chem Lett. 2024 Feb 27;15(3):316-317, PMID: 38505848 |
| Drug discovery in Africa tackles zoonotic and related infections. Hikaambo CN, Shakela N, Woodland JG, Wicht KJ, Chibale K. Sci Transl Med. 2023 Oct 18;15 (718), PMID: 37851825 |
| Antimalarial drug discovery: progress and approaches. Siqueira-Neto JL, Wicht KJ, Chibale K, Burrows JN, Fidock DA, Winzeler EA. Nat Rev Drug Discov. 2023 Oct;22(10):807-826, PMID: 37652975 |
| First fully-automated AI/ML virtual screening cascade implemented at a drug discovery centre in Africa. Turon G, Hlozek J, Woodland JG, Kumar A, Chibale K, Duran-Frigola M. Nat Commun. 2023 Sep 15;14(1):5736, PMID: 37714843 |
| Developing kinase inhibitors for malaria: an opportunity or liability? Mogwera KSP, Chibale K, Arendse LB. Trends Parasitol. 2023 Sep;39(9):720-731, PMID: 37385921 |
| Anti-infectives Developed as Racemic Drugs in the 21st Century: Norm or Exception? Cabrera DG, Smith DA, Basarab GS, Duffy J, Spangenberg T, Chibale K. ACS Med Chem Lett. 2023 Jun 12;14(7):875-878. PMID: 37465315 |
| Including African data in drug discovery and development. Veale CGL, Edkins AL, Winks S, Njoroge M, Chibale K. Nat Rev Drug Discov. 2023 Jul;22(7):521-522, PMID: 37264173 |
| Integrating Pharmacokinetic-Pharmacodynamic Modeling and Physiologically Based Pharmacokinetic Modeling to Optimize Human Dose Predictions for Plasmodium falciparum Malaria: a Chloroquine Case Study. Redhi D, Mulubwa M, Gibhard L, Chibale K. Antimicrob Agents Chemother. 2023 May 17;67(5):e0134522, PMID: 37010410 |
| The implication of Mycobacterium tuberculosis-mediated metabolism of targeted xenobiotics. Singh V, Dziwornu GA, Chibale K. Nat Rev Chem. 2023 May;7(5):340-354, PMID: 37117810 " |
| Antimalarial Imidazopyridines Incorporating an Intramolecular Hydrogen Bonding Motif: Medicinal Chemistry and Mechanistic Studies. Attram HD, Korkor CM, Taylor D, Njoroge M, Chibale K. ACS Infect Dis. 2023 Apr 14;9(4):928-942. PMID: 36946433 |
| Pyrido-Dibemequine Metabolites Exhibit Improved Druglike Features, Inhibit Hemozoin Formation in Plasmodium falciparum, and Synergize with Clinical Antimalarials. Okombo J, Kumar M, Redhi D, Wicht KJ, Wiesner L, Egan TJ, Chibale K. ACS Infect Dis. 2023 Mar 10;9(3):653-667. PMID: 36802523 |
| A Series of Spiropyrimidinetriones that Enhances DNA Cleavage Mediated by Mycobacterium tuberculosis Gyrase. Byl JAW, Mueller R, Bax B, Basarab GS, Chibale K, Osheroff N. ACS Infect Dis. 2023 Mar 10;9(3):706-715. PMID: 36802491 |
| The 2022 H3D Symposium: Celebrating over a Decade of African-Led Infectious Disease Drug Discovery to Enhance Global Health. Woodland JG, Basarab GS, Mogwera K, Winks S, Chibale K. ACS Infect Dis. 2023 Mar 10;9(3):389-393. PMID: 36762950 |
| Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and In Vivo Efficacy in a Plasmodium berghei Mouse Malaria Infection Model. Mambwe D, Korkor CM, Mabhula A, Ngqumba Z, Cloete C, Kumar M, Barros PL, Leshabane M, Coertzen D, Taylor D, Gibhard L, Njoroge M, Lawrence N, Reader J, Moreira DR, Birkholtz LM, Wittlin S, Egan TJ, Chibale K. J Med Chem. 2022 Dec 22;65(24):16695-16715. PMID: 36507890 |
| 1,3-Diarylpyrazolyl-acylsulfonamides Target HadAB/BC Complex in Mycobacterium tuberculosis. Singh V, Grzegorzewicz AE, Fienberg S, Müller R, Khonde LP, Sanz O, Alfonso S, Urones B, Drewes G, Bantscheff M, Ghidelli-Disse S, Ioerger TR, Angala B, Liu J, Lee RE, Sacchettini JC, Krieger IV, Jackson M, Chibale K, Ghorpade SR. ACS Infect Dis. 2022 Nov 11;8(11):2315-2326. PMID: 36325756 |
| The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages. Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M, Lafuente-Monasterio MJ, Fienberg S, Wambua L, Gachuhi S, Coertzen D, van der Watt M, Reader J, Aswat AS, Erlank E, Venter N, Mittal N, Luth MR, Ottilie S, Winzeler EA, Koekemoer LL, Birkholtz LM, Niles JC, Llinás M, Fidock DA, Chibale K. Sci Transl Med. 2022 Oct 19;14(667):eabo7219. PMID: 36260689 |
| Fluorene-Chloroquine Hybrids: Synthesis, in vitro Antiplasmodial Activity, and Inhibition of Heme Detoxification Machinery of Plasmodium falciparum. Parth, Kaur N, Korkor C, Mobin SM, Chibale K, Singh K. ChemMedChem. 2022 Oct 6;17(19):e202200414. PMID: 36017666 |
| Drug discovery research in Ghana, challenges, current efforts, and the way forward. Amewu RK, Amoateng P, Arthur PK, Asare P, Asiamah I, Boamah D, Darko Otchere I, Dzidzor Amengor C, Ekuadzi E, Chibale K, Farrell SJ, Appiah-Oppong R, Osei-Safo D, David Read K, Hugh Gilbert I, Yeboah-Manu D. PLoS Negl Trop Dis. 2022 Sep 15;16(9):e0010645. PMID: 36107859 |
| Keystone Malaria Symposium 2022: a vibrant discussion of progress made and challenges ahead from drug discovery to treatment. Kanai M, Hagenah LM, Ashley EA, Chibale K, Fidock DA. Trends Parasitol. 2022 Sep;38(9):711-718. PMID: 35864072 |
| Thwarting protein synthesis leads to malaria parasite paralysis. Mayoka G, Woodland JG, Chibale K. Trends Parasitol. 2022 Sep;38(9):719-721. PMID: 35843778 |
| Antimalarial Pyrido[1,2-a]benzimidazoles Exert Strong Parasiticidal Effects by Achieving High Cellular Uptake and Suppressing Heme Detoxification. Sousa CC, Dziwornu GA, Quadros HC, Araujo-Neto JH, Chibale K, Moreira DRM. ACS Infect Dis. 2022 Aug 12;8(8):1700-1710. PMID: 35848708 |
| Innovation Experiences from Africa-Led Drug Discovery at the Holistic Drug Discovery and Development (H3D) Centre. Singh V, Mambwe D, Korkor CM, Chibale K. ACS Med Chem Lett. 2022 Jul 11;13(8):1221-1230. PMID: 35978699 |
| Fostering drug discovery and development in Africa. Winks S, Woodland JG, Pillai G', Chibale K. Nat Med. 2022 Aug;28(8):1523-1526. PMID: 35840729 |
| The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance. Murithi JM, Deni I, Pasaje CFA, Okombo J, Bridgford JL, Gnädig NF, Edwards RL, Yeo T, Mok S, Burkhard AY, Coburn-Flynn O, Istvan ES, Sakata-Kato T, Gomez-Lorenzo MG, Cowell AN, Wicht KJ, Le Manach C, Kalantarov GF, Dey S, Duffey M, Laleu B, Lukens AK, Ottilie S, Vanaerschot M, Trakht IN, Gamo FJ, Wirth DF, Goldberg DE, Odom John AR, Chibale K, Winzeler EA, Niles JC, Fidock DA. Cell Chem Biol. 2022 May 19;29(5):824-839.e6. PMID: 34233174 |
| Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity. Govender P, Müller R, Singh K, Reddy V, Eyermann CJ, Fienberg S, Ghorpade SR, Koekemoer L, Myrick A, Schnappinger D, Engelhart C, Meshanni J, Byl JAW, Osheroff N, Singh V, Chibale K, Basarab GS. J Med Chem. 2022 May 12;65(9):6903-6925. PMID: 35500229 |
| Spiropyrimidinetriones: a Class of DNA Gyrase Inhibitors with Activity against Mycobacterium tuberculosis and without Cross-Resistance to Fluoroquinolones. Govender P, Müller R, Singh K, Reddy V, Eyermann CJ, Fienberg S, Ghorpade SR, Koekemoer L, Myrick A, Schnappinger D, Engelhart C, Meshanni J, Byl JAW, Osheroff N, Singh V, Chibale K, Basarab GS. J Med Chem. 2022 May 12;65(9):6903-6925. PMID: 35500229 |
| The diaryl-imidazopyridazine anti-plasmodial compound, MMV652103, exhibits anti-breast cancer activity. Neumann-Mufweba A, Kimani S, Khan SF, Chibale K, Prince S. EXCLI J. 2022 Apr 4;21:656-679. PMID: 35651652 |
| Probing the Requirements for Dual Angiotensin-Converting Enzyme C-Domain Selective/Neprilysin Inhibition. Arendse LB, Cozier GE, Eyermann CJ, Basarab GS, Schwager SL, Chibale K, Acharya KR, Sturrock ED. J Med Chem. 2022 Feb 24;65(4):3371-3387. PMID: 35113565 |
| Quinine fever. Woodland JG, Chibale K. Nat Chem. 2022 Jan;14(1):112. PMID: 34997226 |
| Chemogenomic Fingerprints Associated with Stage-Specific Gametocytocidal Compound Action against Human Malaria Parasites. Niemand J, van Biljon R, van der Watt M, van Heerden A, Reader J, van Wyk R, Orchard L, Chibale K, Llinás M, Birkholtz LM. ACS Infect Dis. 2021 Oct 8;7(10):2904-2916, PMID: 34569223 |
| 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis. Khonde LP, Müller R, Boyle GA, Reddy V, Nchinda AT, Eyermann CJ, Fienberg S, Singh V, Myrick A, Abay E, Njoroge M, Lawrence N, Su Q, Myers TG, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden PD, Massoudi LM, Robertson GT, Lenaerts AJ, Basarab GS, Ghorpade SR, Chibale K. J Med Chem. 2021, 64(17):12790-12807 |
| Rv0684/fusA1, an Essential Gene, Is the Target of Fusidic Acid and Its Derivatives in Mycobacterium tuberculosis. Singh V, Dziwornu GA, Mabhula A, Chibale K, ACS Infect Dis. 2021, 7(8):2437-2444 |
| Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro. Mambwe D, Kumar M, Ferger R, Taylor D, Njoroge M, Coertzen D, Reader J, van der Watt M, Birkholtz LM, Chibale K. ACS Med Chem Lett. 2021; 12(8):1333-1341. |
| Medicinal Chemistry Out of Africa. Chibale K, Wicht KJ, Woodland JG. J Med Chem. 2021, 64(15):10513-10516 |
| Benzimidazole Derivatives Are Potent against Multiple Life Cycle Stages of Plasmodium falciparum Malaria Parasites. Leshabane M, Dziwornu GA, Coertzen D, Reader J, Moyo P, van der Watt M, Chisanga K, Nsanzubuhoro C, Ferger R, Erlank E, Venter N, Koekemoer L, Chibale K, Birkholtz LM. ACS Infect Dis. 2021, 7(7):1945-1955 |
| Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging. van der Westhuyzen R, Mabhula A, Njaria PM, Müller R, Ngumbu Muhunga D, Taylor D, Lawrence N, Njoroge M, Brunschwig C, Moosa A, Singh V, Rao SPS, Manjunatha UH, Smith PW, Warner DF, Street LJ, Chibale K., J. Med. Chem. 2021, 64 (13), 9444-9457 |
| Strategies to Combat Multi-Drug Resistance in Tuberculosis. V. Singh and K. Chibale* Acc. Chem. Res. 2021, 54, 2361−2376 |
| Expanding the Activity Profile of Pyrido[1,2‑a]benzimidazoles:Synthesis and Evaluation of Novel N1‑1-Phenylethanamine Derivatives against Schistosoma mansoni. A. Probst, K. Chisanga, G. A. Dziwornu, C. Haeberli, J. Keiser*, and K. Chibale.* ACS Infect. Dis. 2021, 7, 1032−1043 |
| MalDA, accelerating the malaria drug discovery pipeline. T. Yang, S. Ottilie, E.S. Istvan, K. P. Godinez-Macias, A. Lukens, B. Baragana, B. Campo, C. Walpole, J. Niles, K. Chibale, K. Dechering, M. Llinas, M. Lee, N. Kato, S. Wyllie, C. McNamara, F.-J.B.Gamo, J. Burrows, D. A. Fidock, D. Goldberg, I. Gilbert, D.F. Wirth and, E. Winzeler.* Trends in Parasitology, 2021, 37 (No. 6/June), 493-507 |
| Developing synergistic drug combinations to restore antibiotic sensitivity in drug-resistant Mycobacterium tuberculosis. C. Omollo*, V. Singh, E. Kigondu, A. Wasuna, P. Agarwal, A. Moosa, T. Ioerger, V. Mizrahi, K. Chibale, and D. Warner*. Antimicrob. Agents Chemother. 2021, 65, (Issue 5) e02554-20 |
| Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains inhibit Microtubule and Hemozoin formation: Structure-Activity Relationship and In Vivo Oral Efficacy Studies. G. A. Dziwornu, D. Coertzen, M. Leshabane, C. M. Korkor, C. K. Cloete, M. Njoroge, L. Gibhard, N. Lawrencee, J. Reader, M. van der Watt, S. Wittlin, L.-M. Birkholtz, and K. Chibale.* J. Med. Chem. 2021, 64, 5198−5215 |
| Antiviral Drug Discovery: Preparing for the Next Pandemic. C. S. Adamson, K. Chibale, R. J. M. Goss, M. Jaspars, D. J. Newman and R. A. Dorrington*. Chem. Soc. Rev., 2021, 50, 3647–3655, DOI: 10.1039/d0cs01118e |
| New Amidated 3,6-diphenylated Imidazopyridazines with Potent Antiplasmodium Activity are Dual Inhibitors of Plasmodium phosphatidylinositol-4-kinase and cGMP-dependent protein kinase. P. Cheuka, L. Centani, L. Arendse, S. Fienberg, L. Wambua, S. Renga, G. Dziwornu, M. Kumar, N. Lawrence, D. Taylor, S. Wittlin, D. Coertzen, J. Reader, M. van der Watt, L.-M. Birkholtz and K. Chibale, ACS Infect. Dis. 2021, 7, 34−46 |
| 1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis. Khonde LP, Müller R, Boyle GA, Reddy V, Nchinda AT, Eyermann CJ, Fienberg S, Singh V, Myrick A, Abay E, Njoroge M, Lawrence N, Su Q, Myers TG, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden PD, Massoudi LM, Robertson GT, Lenaerts AJ, Basarab GS, Ghorpade SR, Chibale K. J Med Chem. 2021, 64(17):12790-12807 |
| Rv0684/fusA1, an Essential Gene, Is the Target of Fusidic Acid and Its Derivatives in Mycobacterium tuberculosis. Singh V, Dziwornu GA, Mabhula A, Chibale K, ACS Infect Dis. 2021, 7(8):2437-2444 |
| Structure-Activity Relationship Studies Reveal New Astemizole Analogues Active against Plasmodium falciparum In Vitro. Mambwe D, Kumar M, Ferger R, Taylor D, Njoroge M, Coertzen D, Reader J, van der Watt M, Birkholtz LM, Chibale K. ACS Med Chem Lett. 2021; 12(8):1333-1341. |
| Medicinal Chemistry Out of Africa. Chibale K, Wicht KJ, Woodland JG. J Med Chem. 2021, 64(15):10513-10516 |
| Benzimidazole Derivatives Are Potent against Multiple Life Cycle Stages of Plasmodium falciparum Malaria Parasites. Leshabane M, Dziwornu GA, Coertzen D, Reader J, Moyo P, van der Watt M, Chisanga K, Nsanzubuhoro C, Ferger R, Erlank E, Venter N, Koekemoer L, Chibale K, Birkholtz LM. ACS Infect Dis. 2021, 7(7):1945-1955 |
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Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging. , J. Med. Chem. 2021, 64 (13), 9444-9457 |
| Strategies to Combat Multi-Drug Resistance in Tuberculosis. V. Singh and K. Chibale* Acc. Chem. Res. 2021, 54, 2361−2376 |
| Expanding the Activity Profile of Pyrido[1,2‑a]benzimidazoles:Synthesis and Evaluation of Novel N1‑1-Phenylethanamine Derivatives against Schistosoma mansoni. A. Probst, K. Chisanga, G. A. Dziwornu, C. Haeberli, J. Keiser*, and K. Chibale.* ACS Infect. Dis. 2021, 7, 1032−1043 |
| MalDA, accelerating the malaria drug discovery pipeline. T. Yang, S. Ottilie, E.S. Istvan, K. P. Godinez-Macias, A. Lukens, B. Baragana, B. Campo, C. Walpole, J. Niles, K. Chibale, K. Dechering, M. Llinas, M. Lee, N. Kato, S. Wyllie, C. McNamara, F.-J.B.Gamo, J. Burrows, D. A. Fidock, D. Goldberg, I. Gilbert, D.F. Wirth and, E. Winzeler.* Trends in Parasitology, 2021, 37 (No. 6/June), 493-507 |
| Developing synergistic drug combinations to restore antibiotic sensitivity in drug-resistant Mycobacterium tuberculosis. C. Omollo*, V. Singh, E. Kigondu, A. Wasuna, P. Agarwal, A. Moosa, T. Ioerger, V. Mizrahi, K. Chibale, and D. Warner*. Antimicrob. Agents Chemother. 2021, 65, (Issue 5) e02554-20 |
| Antimalarial Benzimidazole Derivatives Incorporating Phenolic Mannich Base Side Chains inhibit Microtubule and Hemozoin formation: Structure-Activity Relationship and In Vivo Oral Efficacy Studies. G. A. Dziwornu, D. Coertzen, M. Leshabane, C. M. Korkor, C. K. Cloete, M. Njoroge, L. Gibhard, N. Lawrencee, J. Reader, M. van der Watt, S. Wittlin, L.-M. Birkholtz, and K. Chibale.* J. Med. Chem. 2021, 64, 5198−5215 |
| Antiviral Drug Discovery: Preparing for the Next Pandemic. C. S. Adamson, K. Chibale, R. J. M. Goss, M. Jaspars, D. J. Newman and R. A. Dorrington*. Chem. Soc. Rev., 2021, 50, 3647–3655, DOI: 10.1039/d0cs01118e |
| Plasmodium Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities. L. Arendse*, S. Wyllie, K. Chibale and I.H. Gilbert.* ACS Infect. Dis. 2021, 7, 518−534 |
| New Amidated 3,6-diphenylated Imidazopyridazines with Potent Antiplasmodium Activity are Dual Inhibitors of Plasmodium phosphatidylinositol-4-kinase and cGMP-dependent protein kinase. P. Cheuka, L. Centani, L. Arendse, S. Fienberg, L. Wambua, S. Renga, G. Dziwornu, M. Kumar, N. Lawrence, D. Taylor, S. Wittlin, D. Coertzen, J. Reader, M. van der Watt, L.-M. Birkholtz and K. Chibale.*, ACS Infect. Dis. 2021, 7, 34−46 |