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Page 1
Discovery of a Potent and Orally Bioavailable Zwitterionic Series of Selective Estrogen Receptor Degrader-Antagonists.
Scott JS, Stead D, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Cureton N, Davey PRJ, Fisher DI, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Hughes SJ, Hunt TA, Johnson T, Kavanagh SL, Klinowska TCM, Larner CJB, Lawson M, Lister AS, Longmire D, Marden S, McGuire TM, McMillan C, McMurray L, Morrow CJ, Nissink JWM, Moss TA, O'Donovan DH, Polanski R, Stokes S, Thakur K, Trueman D, Truman C, Tucker MJ, Wang H, Whalley N, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. Among authors: barlaam b. J Med Chem. 2023 Feb 23;66(4):2918-2945. doi: 10.1021/acs.jmedchem.2c01964. Epub 2023 Feb 1. J Med Chem. 2023. PMID: 36727211
Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Ballard P, Barlaam BC, Bradbury RH, Dishington A, Hennequin LF, Hickinson DM, Hollingsworth IM, Kettle JG, Klinowska T, Ogilvie DJ, Pearson SE, Scott JS, Suleman A, Whittaker R, Williams EJ, Wood R, Wright L. Ballard P, et al. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6326-9. doi: 10.1016/j.bmcl.2007.08.073. Epub 2007 Sep 2. Bioorg Med Chem Lett. 2007. PMID: 17869514
A new series of neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Barlaam B, Ballard P, Bradbury RH, Ducray R, Germain H, Hickinson DM, Hudson K, Kettle JG, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Pearson SE, Scott JS, Suleman A, Trigwell CB, Vautier M, Whittaker RD, Wood R. Barlaam B, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):674-8. doi: 10.1016/j.bmcl.2007.11.052. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061446
Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
Barlaam B, Acton DG, Ballard P, Bradbury RH, Cross D, Ducray R, Germain H, Hudson K, Klinowska T, Magnien F, Ogilvie DJ, Olivier A, Ross HS, Smith R, Trigwell CB, Vautier M, Wright L. Barlaam B, et al. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1799-803. doi: 10.1016/j.bmcl.2008.02.035. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18313293
Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Péru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N. Barlaam B, et al. J Med Chem. 2015 Jan 22;58(2):943-62. doi: 10.1021/jm501629p. Epub 2015 Jan 7. J Med Chem. 2015. PMID: 25514658
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL, Holmes JL, Howard T, Huang J, Ioannidis S, Kazmirski S, Lamb ML, McGuire TM, Moore JE, Ogg D, Patel A, Pike KG, Pontz T, Robb GR, Su N, Wang H, Wu X, Zhang HJ, Zhang Y, Zheng X, Wang T. Johannes JW, et al. Among authors: barlaam b. ACS Med Chem Lett. 2015 Jan 13;6(3):254-9. doi: 10.1021/ml5003663. eCollection 2015 Mar 12. ACS Med Chem Lett. 2015. PMID: 25815142 Free PMC article.
Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.
Barlaam B, Cosulich S, Delouvrié B, Ellston R, Fitzek M, Germain H, Green S, Hancox U, Harris CS, Hudson K, Lambert-van der Brempt C, Lebraud H, Magnien F, Lamorlette M, Le Griffon A, Morgentin R, Ouvry G, Page K, Pasquet G, Polanska U, Ruston L, Saleh T, Vautier M, Ward L. Barlaam B, et al. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62. doi: 10.1016/j.bmcl.2015.10.002. Epub 2015 Oct 9. Bioorg Med Chem Lett. 2015. PMID: 26475521
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Degorce SL, Barlaam B, Cadogan E, Dishington A, Ducray R, Glossop SC, Hassall LA, Lach F, Lau A, McGuire TM, Nowak T, Ouvry G, Pike KG, Thomason AG. Degorce SL, et al. Among authors: barlaam b. J Med Chem. 2016 Jul 14;59(13):6281-92. doi: 10.1021/acs.jmedchem.6b00519. Epub 2016 Jun 16. J Med Chem. 2016. PMID: 27259031
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Ellston R, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Plé P, Ward L, Warin N. Barlaam B, et al. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954. doi: 10.1016/j.bmcl.2017.03.027. Epub 2017 Mar 14. Bioorg Med Chem Lett. 2017. PMID: 28347666
41 results