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Page 1
Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.
Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T. Baell JB, et al. Among authors: charman sa. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis.
Ferrins L, Rahmani R, Sykes ML, Jones AJ, Avery VM, Teston E, Almohaywi B, Yin J, Smith J, Hyland C, White KL, Ryan E, Campbell M, Charman SA, Kaiser M, Baell JB. Ferrins L, et al. Among authors: charman sa. Eur J Med Chem. 2013 Aug;66:450-65. doi: 10.1016/j.ejmech.2013.05.007. Epub 2013 May 16. Eur J Med Chem. 2013. PMID: 23831695
A novel multiple-stage antimalarial agent that inhibits protein synthesis.
Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH. Baragaña B, et al. Among authors: charman sa. Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Nature. 2015. PMID: 26085270 Free PMC article.
6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors.
Rahmani R, Ban K, Jones AJ, Ferrins L, Ganame D, Sykes ML, Avery VM, White KL, Ryan E, Kaiser M, Charman SA, Baell JB. Rahmani R, et al. Among authors: charman sa. J Med Chem. 2015 Sep 10;58(17):6753-65. doi: 10.1021/acs.jmedchem.5b00438. Epub 2015 Aug 30. J Med Chem. 2015. PMID: 26247439
Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).
Wang C, Zhao Q, Vargas M, Jones JO, White KL, Shackleford DM, Chen G, Saunders J, Ng AC, Chiu FC, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wang C, et al. Among authors: charman sa. J Med Chem. 2016 Dec 8;59(23):10705-10718. doi: 10.1021/acs.jmedchem.6b01410. Epub 2016 Nov 28. J Med Chem. 2016. PMID: 27933964 Free PMC article.
Progress in antischistosomal N,N'-diaryl urea SAR.
Wu J, Wang C, Leas D, Vargas M, White KL, Shackleford DM, Chen G, Sanford AG, Hemsley RM, Davis PH, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wu J, et al. Among authors: charman sa. Bioorg Med Chem Lett. 2018 Feb 1;28(3):244-248. doi: 10.1016/j.bmcl.2017.12.064. Epub 2017 Dec 29. Bioorg Med Chem Lett. 2018. PMID: 29317164 Free PMC article.
SAR of a new antischistosomal urea carboxylic acid.
Wu J, Wang C, Häberli C, White KL, Shackleford DM, Chen G, Dong Y, Charman SA, Keiser J, Vennerstrom JL. Wu J, et al. Among authors: charman sa. Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3648-3651. doi: 10.1016/j.bmcl.2018.10.039. Epub 2018 Oct 25. Bioorg Med Chem Lett. 2018. PMID: 30389288 Free PMC article.
194 results