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Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG).
Tsagris DJ, Birchall K, Bouloc N, Large JM, Merritt A, Smiljanic-Hurley E, Wheldon M, Ansell KH, Kettleborough C, Whalley D, Stewart LB, Bowyer PW, Baker DA, Osborne SA. Tsagris DJ, et al. Among authors: birchall k. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3168-3173. doi: 10.1016/j.bmcl.2018.08.028. Epub 2018 Aug 27. Bioorg Med Chem Lett. 2018. PMID: 30174152 Free PMC article.
Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKε kinases.
McIver EG, Bryans J, Birchall K, Chugh J, Drake T, Lewis SJ, Osborne J, Smiljanic-Hurley E, Tsang W, Kamal A, Levy A, Newman M, Taylor D, Arthur JS, Clark K, Cohen P. McIver EG, et al. Among authors: birchall k. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7169-73. doi: 10.1016/j.bmcl.2012.09.063. Epub 2012 Sep 28. Bioorg Med Chem Lett. 2012. PMID: 23099093
Substituted imidazopyridazines are potent and selective inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).
Chapman TM, Osborne SA, Bouloc N, Large JM, Wallace C, Birchall K, Ansell KH, Jones HM, Taylor D, Clough B, Green JL, Holder AA. Chapman TM, et al. Among authors: birchall k. Bioorg Med Chem Lett. 2013 May 15;23(10):3064-9. doi: 10.1016/j.bmcl.2013.03.017. Epub 2013 Mar 21. Bioorg Med Chem Lett. 2013. PMID: 23570789 Free PMC article.
Biochemical and antiparasitic properties of inhibitors of the Plasmodium falciparum calcium-dependent protein kinase PfCDPK1.
Ansell KH, Jones HM, Whalley D, Hearn A, Taylor DL, Patin EC, Chapman TM, Osborne SA, Wallace C, Birchall K, Large J, Bouloc N, Smiljanic-Hurley E, Clough B, Moon RW, Green JL, Holder AA. Ansell KH, et al. Among authors: birchall k. Antimicrob Agents Chemother. 2014 Oct;58(10):6032-43. doi: 10.1128/AAC.02959-14. Epub 2014 Jul 28. Antimicrob Agents Chemother. 2014. PMID: 25070106 Free PMC article.
A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.
Baker DA, Stewart LB, Large JM, Bowyer PW, Ansell KH, Jiménez-Díaz MB, El Bakkouri M, Birchall K, Dechering KJ, Bouloc NS, Coombs PJ, Whalley D, Harding DJ, Smiljanic-Hurley E, Wheldon MC, Walker EM, Dessens JT, Lafuente MJ, Sanz LM, Gamo FJ, Ferrer SB, Hui R, Bousema T, Angulo-Barturén I, Merritt AT, Croft SL, Gutteridge WE, Kettleborough CA, Osborne SA. Baker DA, et al. Among authors: birchall k. Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x. Nat Commun. 2017. PMID: 28874661 Free PMC article.
Characterization of Three Druggable Hot-Spots in the Aurora-A/TPX2 Interaction Using Biochemical, Biophysical, and Fragment-Based Approaches.
McIntyre PJ, Collins PM, Vrzal L, Birchall K, Arnold LH, Mpamhanga C, Coombs PJ, Burgess SG, Richards MW, Winter A, Veverka V, Delft FV, Merritt A, Bayliss R. McIntyre PJ, et al. Among authors: birchall k. ACS Chem Biol. 2017 Nov 17;12(11):2906-2914. doi: 10.1021/acschembio.7b00537. Epub 2017 Oct 30. ACS Chem Biol. 2017. PMID: 29045126 Free article.
Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines.
Large JM, Birchall K, Bouloc NS, Merritt AT, Smiljanic-Hurley E, Tsagris DJ, Wheldon MC, Ansell KH, Coombs PJ, Kettleborough CA, Whalley D, Stewart LB, Bowyer PW, Baker DA, Osborne SA. Large JM, et al. Among authors: birchall k. Bioorg Med Chem Lett. 2019 Feb 1;29(3):509-514. doi: 10.1016/j.bmcl.2018.11.039. Epub 2018 Nov 20. Bioorg Med Chem Lett. 2019. PMID: 30553738 Free PMC article.
104 results