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Page 1
Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.
Thomas MG, McGonagle K, Rowland P, Robinson DA, Dodd PG, Camino-Díaz I, Campbell L, Cantizani J, Castañeda P, Conn D, Craggs PD, Edwards D, Ferguson L, Fosberry A, Frame L, Goswami P, Hu X, Korczynska J, MacLean L, Martin J, Mutter N, Osuna-Cabello M, Paterson C, Peña I, Pinto EG, Pont C, Riley J, Shishikura Y, Simeons FRC, Stojanovski L, Thomas J, Wrobel K, Young RJ, Zmuda F, Zuccotto F, Read KD, Gilbert IH, Marco M, Miles TJ, Manzano P, De Rycker M. Thomas MG, et al. Among authors: thomas j. J Med Chem. 2023 Aug 10;66(15):10413-10431. doi: 10.1021/acs.jmedchem.3c00582. Epub 2023 Jul 28. J Med Chem. 2023. PMID: 37506194 Free PMC article.
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
Brand S, Ko EJ, Viayna E, Thompson S, Spinks D, Thomas M, Sandberg L, Francisco AF, Jayawardhana S, Smith VC, Jansen C, De Rycker M, Thomas J, MacLean L, Osuna-Cabello M, Riley J, Scullion P, Stojanovski L, Simeons FRC, Epemolu O, Shishikura Y, Crouch SD, Bakshi TS, Nixon CJ, Reid IH, Hill AP, Underwood TZ, Hindley SJ, Robinson SA, Kelly JM, Fiandor JM, Wyatt PG, Marco M, Miles TJ, Read KD, Gilbert IH. Brand S, et al. J Med Chem. 2017 Sep 14;60(17):7284-7299. doi: 10.1021/acs.jmedchem.7b00463. Epub 2017 Aug 27. J Med Chem. 2017. PMID: 28844141 Free PMC article.
Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.
Thomas MG, De Rycker M, Ajakane M, Albrecht S, Álvarez-Pedraglio AI, Boesche M, Brand S, Campbell L, Cantizani-Perez J, Cleghorn LAT, Copley RCB, Crouch SD, Daugan A, Drewes G, Ferrer S, Ghidelli-Disse S, Gonzalez S, Gresham SL, Hill AP, Hindley SJ, Lowe RM, MacKenzie CJ, MacLean L, Manthri S, Martin F, Miguel-Siles J, Nguyen VL, Norval S, Osuna-Cabello M, Woodland A, Patterson S, Pena I, Quesada-Campos MT, Reid IH, Revill C, Riley J, Ruiz-Gomez JR, Shishikura Y, Simeons FRC, Smith A, Smith VC, Spinks D, Stojanovski L, Thomas J, Thompson S, Underwood T, Gray DW, Fiandor JM, Gilbert IH, Wyatt PG, Read KD, Miles TJ. Thomas MG, et al. Among authors: thomas j. J Med Chem. 2019 Feb 14;62(3):1180-1202. doi: 10.1021/acs.jmedchem.8b01218. Epub 2018 Dec 20. J Med Chem. 2019. PMID: 30570265 Free PMC article.
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity.
Thomas MG, De Rycker M, Wall RJ, Spinks D, Epemolu O, Manthri S, Norval S, Osuna-Cabello M, Patterson S, Riley J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Naylor C, Fiandor JM, Wyatt PG, Marco M, Wyllie S, Read KD, Miles TJ, Gilbert IH. Thomas MG, et al. Among authors: thomas j. J Med Chem. 2020 Sep 10;63(17):9523-9539. doi: 10.1021/acs.jmedchem.0c00705. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32663005 Free PMC article.
Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis.
Thomas MG, De Rycker M, Ajakane M, Crouch SD, Campbell L, Daugan A, Fra G, Guerrero C, Mackenzie CJ, MacLean L, Manthri S, Martin F, Norval S, Osuna-Cabello M, Riley J, Shishikura Y, Miguel-Siles J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Velasco RF, Fiandor JM, Wyatt PG, Read KD, Gilbert IH, Miles TJ. Thomas MG, et al. Among authors: thomas j. RSC Med Chem. 2020 Aug 6;11(10):1168-1177. doi: 10.1039/d0md00203h. eCollection 2020 Oct 1. RSC Med Chem. 2020. PMID: 33479621 Free PMC article.
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Thomas M, Brand S, De Rycker M, Zuccotto F, Lukac I, Dodd PG, Ko EJ, Manthri S, McGonagle K, Osuna-Cabello M, Riley J, Pont C, Simeons F, Stojanovski L, Thomas J, Thompson S, Viayna E, Fiandor JM, Martin J, Wyatt PG, Miles TJ, Read KD, Marco M, Gilbert IH. Thomas M, et al. J Med Chem. 2021 May 13;64(9):5905-5930. doi: 10.1021/acs.jmedchem.1c00047. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904304 Free PMC article.
Identification and development of a series of disubstituted piperazines for the treatment of Chagas disease.
McGonagle K, Tarver GJ, Cantizani J, Cotillo I, Dodd PG, Ferguson L, Gilbert IH, Marco M, Miles T, Naylor C, Osuna-Cabello M, Paterson C, Read KD, Pinto EG, Riley J, Scullion P, Shishikura Y, Simeons F, Stojanovski L, Svensen N, Thomas J, Wyatt PG, Manzano P, De Rycker M, Thomas MG. McGonagle K, et al. Among authors: thomas j, thomas mg. Eur J Med Chem. 2022 Aug 5;238:114421. doi: 10.1016/j.ejmech.2022.114421. Epub 2022 May 6. Eur J Med Chem. 2022. PMID: 35594652 Free article.
2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.
Thomas MG, De Rycker M, Cotillo Torrejon I, Thomas J, Riley J, Spinks D, Read KD, Miles TJ, Gilbert IH, Wyatt PG. Thomas MG, et al. Among authors: thomas j. Bioorg Med Chem Lett. 2018 Oct 1;28(18):3025-3030. doi: 10.1016/j.bmcl.2018.08.005. Epub 2018 Aug 3. Bioorg Med Chem Lett. 2018. PMID: 30104093 Free PMC article.
Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.
Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG. Wyllie S, et al. Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8. Proc Natl Acad Sci U S A. 2019. PMID: 30962368 Free PMC article.
The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani.
Wall RJ, Carvalho S, Milne R, Bueren-Calabuig JA, Moniz S, Cantizani-Perez J, MacLean L, Kessler A, Cotillo I, Sastry L, Manthri S, Patterson S, Zuccotto F, Thompson S, Martin J, Marco M, Miles TJ, De Rycker M, Thomas MG, Fairlamb AH, Gilbert IH, Wyllie S. Wall RJ, et al. Among authors: thomas mg. ACS Infect Dis. 2020 Mar 13;6(3):515-528. doi: 10.1021/acsinfecdis.9b00426. Epub 2020 Jan 30. ACS Infect Dis. 2020. PMID: 31967783 Free PMC article.
638 results