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Identification of three new inhibitor classes against Plasmodium falciparum

Sandra Johannsen, Robin M. Gierse, Arne Krüger, Rachel L. Edwards, Vittoria Nanna, Anna Fontana, Di Zhu, Tizina Masini, Lais Pessanha de Carvalho, Mael Poizat, Bart Kieftenbelt, Dana M. Hodge, Sophie Alvarez, Daan Bunt, Kamila Anna Meissner, Edmarcia Elisa de Souza, Melloney Dröge, Bernard van Vliet, Jack de Hartog, Michael C. Hutter, Jana Held, Audrey R. Odom John, Carsten Wrenger, Anna K. H. Hirsch

Version 1 posted 12 April 2022

329

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Biological and Medicinal Chemistry

Working Paper

Multicomponent Syntheses Enable the Discovery of Novel Quisinostat-Derived Chemotypes as Histone Deacetylase Inhibitors

Daniel Stopper, Susanna Buntrock, Kathrin Tan, Lais Pessanha de Carvalho, Linda Schäker-Hübner, Jana Held, Matthias Kassack, Finn Kristian Hansen

Version 2 posted 07 November 2024

125

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Biological and Medicinal Chemistry

Working Paper

Targeting PfCLK3 with Covalent Inhibitors: A Novel Strategy for Malaria Treatment

Andrew Jamieson, Skye Brettell, Omar Jahna, Abbey Begen, Gillian Cann, Niniola Olaniyan, Saumya Sharma, Tamas Yelland, Alison Hole, Benazir Alam, Ross Gillespie, Michael Capper, Graeme Milligan, David Clarke, Andrew Tobin

Version 1 posted 21 May 2024

387

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Biological and Medicinal Chemistry

Working Paper

Exploring Alternative Zinc-Binding Groups in Histone Deacetylase (HDAC) Inhibitors Uncovers DS-103 as a Potent Ethylhydrazide-Based HDAC Inhibitor with Chemosensitizing Properties

Daniel Stopper, Lukas Biermann, Paris Watson, jingyu Li, Beate König, Matthew Gaynes, Lais Pessanha de Carvalho, Maria Hanl, Alexandra Hamacher, Linda Schäker-Hübner, Jana Held, David Christianson, Matthias Kassack, Finn Kristian Hansen

Version 1 posted 01 October 2024

264

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Biological and Medicinal Chemistry

Working Paper

Characterization of 2,4-dianilinopyrimidines Against Five P. falciparum Kinases PfARK1, PfARK3, PfNEK3, PfPK9 and PfPKB

Han Wee Ong, Chandi de Silva, Krisha Avalani, Frank Kwarcinski, Christopher Mansfield, Michael Chirgwin, Anna Truong, Emily Derbyshire, Reena Zutshi, David Drewry

Version 1 posted 10 August 2023

144

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Biological and Medicinal Chemistry

Working Paper

Development of Potent and Selective PfCLK3 Inhibitors Based on GSK-TCMDC151 as a New Class of Antimalarials

Amit Mahindra, Omar Janha, Kopano Mapesa, Ana Sanchez-Azqueta, Mahmood M. Alam, Andrew Tobin, Andrew Jamieson

Version 1 posted 13 September 2019

804

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Biological and Medicinal Chemistry

Working Paper

Half- Sandwich cyclopentadienylruthenium(II) Complexes: A New Antimalarial Chemotype

Sofia Alexandra Milheiro, Joana Gonçalves, Ricardo Lopes, Margarida Madureira, Lis Lobo, Andreia Lopes, Fatima Nogueira, Diana Fontinha, Miguel Prudêncio, Fátima Piedade, Sandra Pinto, Pedro Florindo, Rui Moreira

Version 1 posted 21 April 2020

510

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Biological and Medicinal Chemistry

Working Paper

Exploring aspartic protease inhibitor binding to design selective antimalarials

Raitis Bobrovs, Emils Basens, Laura Drunka, Iveta Kanepe, Sofija Matisone, Karlis Velins, Victor Andrianov, Gundars Leitis, Diana Zelencova-Gopejenko, Dace Rasina, Aigars Jirgensons, Kristaps Jaudzems

Version 1 posted 31 January 2022

422

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Biological and Medicinal Chemistry

Working Paper

Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity Against Blood Stage Parasites in vitro

Kareem Galal, Anna Truong, Frank Kwarcinski, Chandi de Silva, Krisha Avalani, Tammy Havener, Michael Chirgwin, Eric Merten, Han Wee Ong, Caleb Willis, Ahmad Abdelwaly, Mohamed Helal, Emily Derbyshire, Reena Zutshi, David Drewry

Version 1 posted 17 June 2022

196

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Biological and Medicinal Chemistry

Working Paper

Inhibition of Thiamine Diphosphate (ThDP)-dependent Enzymes by Triazole-based Thiamine Analogues

Alex H. Y. Chan, Terence C. S. Ho, Imam Fathoni, Rebecca Pope, Kevin J. Saliba, Finian James Leeper

Version 1 posted 25 January 2023

175

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21 results in Malaria in Keywords: Malaria

Identification of three new inhibitor classes against Plasmodium falciparum

Multicomponent Syntheses Enable the Discovery of Novel Quisinostat-Derived Chemotypes as Histone Deacetylase Inhibitors

Targeting PfCLK3 with Covalent Inhibitors: A Novel Strategy for Malaria Treatment

Exploring Alternative Zinc-Binding Groups in Histone Deacetylase (HDAC) Inhibitors Uncovers DS-103 as a Potent Ethylhydrazide-Based HDAC Inhibitor with Chemosensitizing Properties

Characterization of 2,4-dianilinopyrimidines Against Five P. falciparum Kinases PfARK1, PfARK3, PfNEK3, PfPK9 and PfPKB

Development of Potent and Selective PfCLK3 Inhibitors Based on GSK-TCMDC151 as a New Class of Antimalarials

Half- Sandwich cyclopentadienylruthenium(II) Complexes: A New Antimalarial Chemotype

Exploring aspartic protease inhibitor binding to design selective antimalarials

Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial PfGSK3/PfPK6 with Activity Against Blood Stage Parasites in vitro

Inhibition of Thiamine Diphosphate (ThDP)-dependent Enzymes by Triazole-based Thiamine Analogues

21 results in Keywords: Malaria