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Page 1
1-Methyl-1H-pyrazole-5-carboxamide Derivatives Exhibit Unexpected Acute Mammalian Toxicity.
Preston S, Garcia-Bustos J, Hall LG, Martin SD, Le TG, Kundu A, Ghoshal A, Nguyen NH, Jiao Y, Ruan B, Xue L, Huang F, Chang BCH, McGee SL, Wells TNC, Palmer MJ, Jabbar A, Gasser RB, Baell JB. Preston S, et al. Among authors: nguyen nh. J Med Chem. 2021 Jan 14;64(1):840-844. doi: 10.1021/acs.jmedchem.0c01793. Epub 2020 Dec 22. J Med Chem. 2021. PMID: 33352050
Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides.
Russell S, Rahmani R, Jones AJ, Newson HL, Neilde K, Cotillo I, Rahmani Khajouei M, Ferrins L, Qureishi S, Nguyen N, Martinez-Martinez MS, Weaver DF, Kaiser M, Riley J, Thomas J, De Rycker M, Read KD, Flematti GR, Ryan E, Tanghe S, Rodriguez A, Charman SA, Kessler A, Avery VM, Baell JB, Piggott MJ. Russell S, et al. J Med Chem. 2016 Nov 10;59(21):9686-9720. doi: 10.1021/acs.jmedchem.6b00442. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27548560 Free article.
GSTO1-1 plays a pro-inflammatory role in models of inflammation, colitis and obesity.
Menon D, Innes A, Oakley AJ, Dahlstrom JE, Jensen LM, Brüstle A, Tummala P, Rooke M, Casarotto MG, Baell JB, Nguyen N, Xie Y, Cuellar M, Strasser J, Dahlin JL, Walters MA, Burgio G, O'Neill LAJ, Board PG. Menon D, et al. Sci Rep. 2017 Dec 19;7(1):17832. doi: 10.1038/s41598-017-17861-6. Sci Rep. 2017. PMID: 29259211 Free PMC article.
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. Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1. Nature. 2018. PMID: 30069049
Optimization of Novel 1-Methyl-1 H-Pyrazole-5-carboxamides Leads to High Potency Larval Development Inhibitors of the Barber's Pole Worm.
Le TG, Kundu A, Ghoshal A, Nguyen NH, Preston S, Jiao Y, Ruan B, Xue L, Huang F, Keiser J, Hofmann A, Chang BCH, Garcia-Bustos J, Jabbar A, Wells TNC, Palmer MJ, Gasser RB, Baell JB. Le TG, et al. Among authors: nguyen nh. J Med Chem. 2018 Dec 13;61(23):10875-10894. doi: 10.1021/acs.jmedchem.8b01544. Epub 2018 Nov 29. J Med Chem. 2018. PMID: 30403349
Structure-Activity Relationship Studies of Tolfenpyrad Reveal Subnanomolar Inhibitors of Haemonchus contortus Development.
Le TG, Kundu A, Ghoshal A, Nguyen NH, Preston S, Jiao Y, Ruan B, Xue L, Huang F, Keiser J, Hofmann A, Chang BCH, Garcia-Bustos J, Wells TNC, Palmer MJ, Jabbar A, Gasser RB, Baell JB. Le TG, et al. Among authors: nguyen nh. J Med Chem. 2019 Jan 24;62(2):1036-1053. doi: 10.1021/acs.jmedchem.8b01789. Epub 2019 Jan 7. J Med Chem. 2019. PMID: 30571110
Tetrahydroquinoxalines induce a lethal evisceration phenotype in Haemonchus contortus in vitro.
Jiao Y, Preston S, Garcia-Bustos JF, Baell JB, Ventura S, Le T, McNamara N, Nguyen N, Botteon A, Skinner C, Danne J, Ellis S, Koehler AV, Wang T, Chang BCH, Hofmann A, Jabbar A, Gasser RB. Jiao Y, et al. Int J Parasitol Drugs Drug Resist. 2019 Apr;9:59-71. doi: 10.1016/j.ijpddr.2018.12.007. Epub 2018 Dec 30. Int J Parasitol Drugs Drug Resist. 2019. PMID: 30690282 Free PMC article.
Singlet molecular oxygen regulates vascular tone and blood pressure in inflammation.
Stanley CP, Maghzal GJ, Ayer A, Talib J, Giltrap AM, Shengule S, Wolhuter K, Wang Y, Chadha P, Suarna C, Prysyazhna O, Scotcher J, Dunn LL, Prado FM, Nguyen N, Odiba JO, Baell JB, Stasch JP, Yamamoto Y, Di Mascio P, Eaton P, Payne RJ, Stocker R. Stanley CP, et al. Nature. 2019 Feb;566(7745):548-552. doi: 10.1038/s41586-019-0947-3. Epub 2019 Feb 13. Nature. 2019. PMID: 30760924
568 results