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An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes.
Albert JS, Blomberg N, Breeze AL, Brown AJ, Burrows JN, Edwards PD, Folmer RH, Geschwindner S, Griffen EJ, Kenny PW, Nowak T, Olsson LL, Sanganee H, Shapiro AB. Albert JS, et al. Among authors: burrows jn. Curr Top Med Chem. 2007;7(16):1600-29. doi: 10.2174/156802607782341091. Curr Top Med Chem. 2007. PMID: 17979771 Review.
Fragment screening: an introduction.
Leach AR, Hann MM, Burrows JN, Griffen EJ. Leach AR, et al. Among authors: burrows jn. Mol Biosyst. 2006 Sep;2(9):430-46. doi: 10.1039/b610069b. Mol Biosyst. 2006. PMID: 17153140
ProSAR: a new methodology for combinatorial library design.
Chen H, Börjesson U, Engkvist O, Kogej T, Svensson MA, Blomberg N, Weigelt D, Burrows JN, Lange T. Chen H, et al. Among authors: burrows jn. J Chem Inf Model. 2009 Mar;49(3):603-14. doi: 10.1021/ci800231d. J Chem Inf Model. 2009. PMID: 19434898
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
Gujjar R, El Mazouni F, White KL, White J, Creason S, Shackleford DM, Deng X, Charman WN, Bathurst I, Burrows J, Floyd DM, Matthews D, Buckner FS, Charman SA, Phillips MA, Rathod PK. Gujjar R, et al. J Med Chem. 2011 Jun 9;54(11):3935-49. doi: 10.1021/jm200265b. Epub 2011 May 12. J Med Chem. 2011. PMID: 21517059 Free PMC article.
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.
Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA, Charron CL, Bruzzese F, Yang X, Zhao X, Huang SC, Hutton CA, Burrows JN, Winzeler EA, Avery VM, Dick LR, Tilley L. Xie SC, et al. Among authors: burrows jn. J Med Chem. 2018 Nov 21;61(22):10053-10066. doi: 10.1021/acs.jmedchem.8b01161. Epub 2018 Nov 7. J Med Chem. 2018. PMID: 30373366 Free PMC article.
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J, Crighton E, Chen G, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Huertas-Valentin L, Martinez-Martinez MS, Lafuente-Monasterio MJ, Chittimalla R, Shahi SP, Wittlin S, Waterson D, Burrows JN, Matthews D, Tomchick D, Rathod PK, Palmer MJ, Charman SA, Phillips MA. Kokkonda S, et al. Among authors: burrows jn. J Med Chem. 2020 May 14;63(9):4929-4956. doi: 10.1021/acs.jmedchem.0c00311. Epub 2020 Apr 16. J Med Chem. 2020. PMID: 32248693 Free PMC article.
Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.
Van Voorhis WC, Adams JH, Adelfio R, Ahyong V, Akabas MH, Alano P, Alday A, Alemán Resto Y, Alsibaee A, Alzualde A, Andrews KT, Avery SV, Avery VM, Ayong L, Baker M, Baker S, Ben Mamoun C, Bhatia S, Bickle Q, Bounaadja L, Bowling T, Bosch J, Boucher LE, Boyom FF, Brea J, Brennan M, Burton A, Caffrey CR, Camarda G, Carrasquilla M, Carter D, Belen Cassera M, Chih-Chien Cheng K, Chindaudomsate W, Chubb A, Colon BL, Colón-López DD, Corbett Y, Crowther GJ, Cowan N, D'Alessandro S, Le Dang N, Delves M, DeRisi JL, Du AY, Duffy S, Abd El-Salam El-Sayed S, Ferdig MT, Fernández Robledo JA, Fidock DA, Florent I, Fokou PV, Galstian A, Gamo FJ, Gokool S, Gold B, Golub T, Goldgof GM, Guha R, Guiguemde WA, Gural N, Guy RK, Hansen MA, Hanson KK, Hemphill A, Hooft van Huijsduijnen R, Horii T, Horrocks P, Hughes TB, Huston C, Igarashi I, Ingram-Sieber K, Itoe MA, Jadhav A, Naranuntarat Jensen A, Jensen LT, Jiang RH, Kaiser A, Keiser J, Ketas T, Kicka S, Kim S, Kirk K, Kumar VP, Kyle DE, Lafuente MJ, Landfear S, Lee N, Lee S, Lehane AM, Li F, Little D, Liu L, Llinás M, Loza MI, Lubar A, Lucantoni L, Lucet I, Maes L, Mancama D, Mansour NR, March S, McGowan S, Medina Vera I, Meister S, Mercer L, Mestr… See abstract for full author list ➔ Van Voorhis WC, et al. PLoS Pathog. 2016 Jul 28;12(7):e1005763. doi: 10.1371/journal.ppat.1005763. eCollection 2016 Jul. PLoS Pathog. 2016. PMID: 27467575 Free PMC article.
101 results