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Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.
Wagman AS, Boyce RS, Brown SP, Fang E, Goff D, Jansen JM, Le VP, Levine BH, Ng SC, Ni ZJ, Nuss JM, Pfister KB, Ramurthy S, Renhowe PA, Ring DB, Shu W, Subramanian S, Zhou XA, Shafer CM, Harrison SD, Johnson KW, Bussiere DE. Wagman AS, et al. Among authors: bussiere de. J Med Chem. 2017 Oct 26;60(20):8482-8514. doi: 10.1021/acs.jmedchem.7b00922. Epub 2017 Oct 10. J Med Chem. 2017. PMID: 29016121
Design and structure-activity relationship of heterocyclic analogs of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones as inhibitors of receptor tyrosine kinases.
Frazier K, Jazan E, McBride CM, Pecchi S, Renhowe PA, Shafer CM, Taylor C, Bussiere D, He MM, Jansen JM, Lapointe G, Ma S, Vora J, Wiesmann M. Frazier K, et al. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2247-51. doi: 10.1016/j.bmcl.2006.01.020. Epub 2006 Jan 30. Bioorg Med Chem Lett. 2006. PMID: 16446087
4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors.
Ni ZJ, Barsanti P, Brammeier N, Diebes A, Poon DJ, Ng S, Pecchi S, Pfister K, Renhowe PA, Ramurthy S, Wagman AS, Bussiere DE, Le V, Zhou Y, Jansen JM, Ma S, Gesner TG. Ni ZJ, et al. Among authors: bussiere de. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3121-4. doi: 10.1016/j.bmcl.2006.03.059. Epub 2006 Apr 5. Bioorg Med Chem Lett. 2006. PMID: 16603354
Discovery and optimization of novel pyridines as highly potent and selective glycogen synthase kinase 3 inhibitors.
Ramurthy S, Pfister KB, Boyce RS, Brown SP, Costales AQ, Desai MC, Fang E, Levine BH, Ng SC, Nuss JM, Ring DB, Shafer CM, Shu W, Subramanian S, Wagman AS, Wang H, Bussiere DE. Ramurthy S, et al. Among authors: bussiere de. Bioorg Med Chem Lett. 2020 Feb 15;30(4):126930. doi: 10.1016/j.bmcl.2019.126930. Epub 2019 Dec 23. Bioorg Med Chem Lett. 2020. PMID: 31926786
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
Burger MT, Pecchi S, Wagman A, Ni ZJ, Knapp M, Hendrickson T, Atallah G, Pfister K, Zhang Y, Bartulis S, Frazier K, Ng S, Smith A, Verhagen J, Haznedar J, Huh K, Iwanowicz E, Xin X, Menezes D, Merritt H, Lee I, Wiesmann M, Kaufman S, Crawford K, Chin M, Bussiere D, Shoemaker K, Zaror I, Maira SM, Voliva CF. Burger MT, et al. ACS Med Chem Lett. 2011 Aug 26;2(10):774-9. doi: 10.1021/ml200156t. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900266 Free PMC article.
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase.
Lingel A, Sendzik M, Huang Y, Shultz MD, Cantwell J, Dillon MP, Fu X, Fuller J, Gabriel T, Gu J, Jiang X, Li L, Liang F, McKenna M, Qi W, Rao W, Sheng X, Shu W, Sutton J, Taft B, Wang L, Zeng J, Zhang H, Zhang M, Zhao K, Lindvall M, Bussiere DE. Lingel A, et al. Among authors: bussiere de. J Med Chem. 2017 Jan 12;60(1):415-427. doi: 10.1021/acs.jmedchem.6b01473. Epub 2017 Jan 3. J Med Chem. 2017. PMID: 27992714
Inhibition of prenylated KRAS in a lipid environment.
Jansen JM, Wartchow C, Jahnke W, Fong S, Tsang T, Pfister K, Zavorotinskaya T, Bussiere D, Cheng JM, Crawford K, Dai Y, Dove J, Fang E, Feng Y, Florent JM, Fuller J, Gossert AD, Hekmat-Nejad M, Henry C, Klopp J, Lenahan WP, Lingel A, Ma S, Meyer A, Mishina Y, Narberes J, Pardee G, Ramurthy S, Rieffel S, Stuart D, Subramanian S, Tandeske L, Widger S, Widmer A, Winterhalter A, Zaror I, Hardy S. Jansen JM, et al. PLoS One. 2017 Apr 6;12(4):e0174706. doi: 10.1371/journal.pone.0174706. eCollection 2017. PLoS One. 2017. PMID: 28384226 Free PMC article.
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
Skepper CK, Armstrong D, Balibar CJ, Bauer D, Bellamacina C, Benton BM, Bussiere D, De Pascale G, De Vicente J, Dean CR, Dhumale B, Fisher LM, Fuller J, Fulsunder M, Holder LM, Hu C, Kantariya B, Lapointe G, Leeds JA, Li X, Lu P, Lvov A, Ma S, Madhavan S, Malekar S, McKenney D, Mergo W, Metzger L, Moser HE, Mutnick D, Noeske J, Osborne C, Patel A, Patel D, Patel T, Prajapati K, Prosen KR, Reck F, Richie DL, Rico A, Sanderson MR, Satasia S, Sawyer WS, Selvarajah J, Shah N, Shanghavi K, Shu W, Thompson KV, Traebert M, Vala A, Vala L, Veselkov DA, Vo J, Wang M, Widya M, Williams SL, Xu Y, Yue Q, Zang R, Zhou B, Rivkin A. Skepper CK, et al. Among authors: de pascale g, bussiere d, de vicente j. J Med Chem. 2020 Jul 23;63(14):7773-7816. doi: 10.1021/acs.jmedchem.0c00347. Epub 2020 Jul 7. J Med Chem. 2020. PMID: 32634310
45 results