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Page 1
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.
LaMarche MJ, Leeds JA, Amaral K, Brewer JT, Bushell SM, Dewhurst JM, Dzink-Fox J, Gangl E, Goldovitz J, Jain A, Mullin S, Neckermann G, Osborne C, Palestrant D, Patane MA, Rann EM, Sachdeva M, Shao J, Tiamfook S, Whitehead L, Yu D. LaMarche MJ, et al. Among authors: gangl e. J Med Chem. 2011 Dec 8;54(23):8099-109. doi: 10.1021/jm200938f. Epub 2011 Nov 1. J Med Chem. 2011. PMID: 21999529
A new structural alert for benzimidazoles: 2,6-dimethylphenyl substituents increase mutagenic potential and time-dependent CYP3A4 inhibition risk.
Kwak Y, Coppola G, Forster CJ, Gilmore TA, Gong Y, Kanter A, Neubert A, Stroup B, Szklennik P, Glowienke S, Stadelmann P, Bell L, Bickford S, Gangl E, Gunduz M, Jain M, Zhan J, Serrano-Wu MH. Kwak Y, et al. Among authors: gangl e. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1422-4. doi: 10.1016/j.bmcl.2011.01.023. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295471
In vitro and in vivo activities of novel, semisynthetic thiopeptide inhibitors of bacterial elongation factor Tu.
Leeds JA, LaMarche MJ, Brewer JT, Bushell SM, Deng G, Dewhurst JM, Dzink-Fox J, Gangl E, Jain A, Lee L, Lilly M, Manni K, Mullin S, Neckermann G, Osborne C, Palestrant D, Patane MA, Raimondi A, Ranjitkar S, Rann EM, Sachdeva M, Shao J, Tiamfook S, Whitehead L, Yu D. Leeds JA, et al. Among authors: gangl e. Antimicrob Agents Chemother. 2011 Nov;55(11):5277-83. doi: 10.1128/AAC.00582-11. Epub 2011 Aug 8. Antimicrob Agents Chemother. 2011. PMID: 21825297 Free PMC article.
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.
Sutton JM, Clark DE, Dunsdon SJ, Fenton G, Fillmore A, Harris NV, Higgs C, Hurley CA, Krintel SL, MacKenzie RE, Duttaroy A, Gangl E, Maniara W, Sedrani R, Namoto K, Ostermann N, Gerhartz B, Sirockin F, Trappe J, Hassiepen U, Baeschlin DK. Sutton JM, et al. Among authors: gangl e. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1464-8. doi: 10.1016/j.bmcl.2011.11.054. Epub 2011 Nov 20. Bioorg Med Chem Lett. 2012. PMID: 22177783
Antibiotic optimization and chemical structure stabilization of thiomuracin A.
LaMarche MJ, Leeds JA, Dzink-Fox J, Gangl E, Krastel P, Neckermann G, Palestrant D, Patane MA, Rann EM, Tiamfook S, Yu D. LaMarche MJ, et al. Among authors: gangl e. J Med Chem. 2012 Aug 9;55(15):6934-41. doi: 10.1021/jm300783c. Epub 2012 Jul 31. J Med Chem. 2012. PMID: 22812377
Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors.
Papillon JP, Adams CM, Hu QY, Lou C, Singh AK, Zhang C, Carvalho J, Rajan S, Amaral A, Beil ME, Fu F, Gangl E, Hu CW, Jeng AY, LaSala D, Liang G, Logman M, Maniara WM, Rigel DF, Smith SA, Ksander GM. Papillon JP, et al. Among authors: gangl e. J Med Chem. 2015 Jun 11;58(11):4749-70. doi: 10.1021/acs.jmedchem.5b00407. Epub 2015 May 21. J Med Chem. 2015. PMID: 25953419
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.
Scott JS, Moss TA, Balazs A, Barlaam B, Breed J, Carbajo RJ, Chiarparin E, Davey PRJ, Delpuech O, Fawell S, Fisher DI, Gagrica S, Gangl ET, Grebe T, Greenwood RD, Hande S, Hatoum-Mokdad H, Herlihy K, Hughes S, Hunt TA, Huynh H, Janbon SLM, Johnson T, Kavanagh S, Klinowska T, Lawson M, Lister AS, Marden S, McGinnity DF, Morrow CJ, Nissink JWM, O'Donovan DH, Peng B, Polanski R, Stead DS, Stokes S, Thakur K, Throner SR, Tucker MJ, Varnes J, Wang H, Wilson DM, Wu D, Wu Y, Yang B, Yang W. Scott JS, et al. Among authors: gangl et. J Med Chem. 2020 Dec 10;63(23):14530-14559. doi: 10.1021/acs.jmedchem.0c01163. Epub 2020 Sep 29. J Med Chem. 2020. PMID: 32910656
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: gangl et. 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
In vivo validation of thymidylate kinase (TMK) with a rationally designed, selective antibacterial compound.
Keating TA, Newman JV, Olivier NB, Otterson LG, Andrews B, Boriack-Sjodin PA, Breen JN, Doig P, Dumas J, Gangl E, Green OM, Guler SY, Hentemann MF, Joseph-McCarthy D, Kawatkar S, Kutschke A, Loch JT, McKenzie AR, Pradeepan S, Prasad S, Martínez-Botella G. Keating TA, et al. Among authors: gangl e. ACS Chem Biol. 2012 Nov 16;7(11):1866-72. doi: 10.1021/cb300316n. Epub 2012 Aug 28. ACS Chem Biol. 2012. PMID: 22908966
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: gangl e. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
36 results