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Page 1
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. Among authors: fiandor jm. 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.
Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series.
Coterón JM, Catterick D, Castro J, Chaparro MJ, Díaz B, Fernández E, Ferrer S, Gamo FJ, Gordo M, Gut J, de las Heras L, Legac J, Marco M, Miguel J, Muñoz V, Porras E, de la Rosa JC, Ruiz JR, Sandoval E, Ventosa P, Rosenthal PJ, Fiandor JM. Coterón JM, et al. Among authors: fiandor jm. J Med Chem. 2010 Aug 26;53(16):6129-52. doi: 10.1021/jm100556b. J Med Chem. 2010. PMID: 20672841
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. Among authors: fiandor jm. 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.
Identifying inhibitors of the Leishmania inositol phosphorylceramide synthase with antiprotozoal activity using a yeast-based assay and ultra-high throughput screening platform.
Norcliffe JL, Mina JG, Alvarez E, Cantizani J, de Dios-Anton F, Colmenarejo G, Valle SG, Marco M, Fiandor JM, Martin JJ, Steel PG, Denny PW. Norcliffe JL, et al. Among authors: fiandor jm. Sci Rep. 2018 Mar 2;8(1):3938. doi: 10.1038/s41598-018-22063-9. Sci Rep. 2018. PMID: 29500420 Free PMC article.
Synthesis and Structure-Activity Relationships of the Novel Antimalarials 5-Pyridinyl-4(1 H)-Pyridones.
Bueno JM, Calderon F, Chicharro J, De la Rosa JC, Díaz B, Fernández J, Fiandor JM, Fraile MT, García M, Herreros E, García-Pérez A, Lorenzo M, Mallo A, Puente M, Saadeddin A, Ferrer S, Angulo-Barturen I, Burrows JN, León ML. Bueno JM, et al. Among authors: fiandor jm. J Med Chem. 2018 Apr 26;61(8):3422-3435. doi: 10.1021/acs.jmedchem.7b01256. Epub 2018 Apr 5. J Med Chem. 2018. PMID: 29589932
Metabolic Clustering Analysis as a Strategy for Compound Selection in the Drug Discovery Pipeline for Leishmaniasis.
Armitage EG, Godzien J, Peña I, López-Gonzálvez Á, Angulo S, Gradillas A, Alonso-Herranz V, Martín J, Fiandor JM, Barrett MP, Gabarro R, Barbas C. Armitage EG, et al. Among authors: fiandor jm. ACS Chem Biol. 2018 May 18;13(5):1361-1369. doi: 10.1021/acschembio.8b00204. Epub 2018 Apr 24. ACS Chem Biol. 2018. PMID: 29671577 Free article.
Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis.
Wyllie S, Thomas M, Patterson S, Crouch S, De Rycker M, Lowe R, Gresham S, Urbaniak MD, Otto TD, Stojanovski L, Simeons FRC, Manthri S, MacLean LM, Zuccotto F, Homeyer N, Pflaumer H, Boesche M, Sastry L, Connolly P, Albrecht S, Berriman M, Drewes G, Gray DW, Ghidelli-Disse S, Dixon S, Fiandor JM, Wyatt PG, Ferguson MAJ, Fairlamb AH, Miles TJ, Read KD, Gilbert IH. Wyllie S, et al. Among authors: fiandor jm. Nature. 2018 Aug;560(7717):192-197. doi: 10.1038/s41586-018-0356-z. Epub 2018 Jul 25. Nature. 2018. PMID: 30046105 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: fiandor jm. 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.
24 results