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Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.
Han W, Menezes DL, Xu Y, Knapp MS, Elling R, Burger MT, Ni ZJ, Smith A, Lan J, Williams TE, Verhagen J, Huh K, Merritt H, Chan J, Kaufman S, Voliva CF, Pecchi S. Han W, et al. Among authors: kaufman s. Bioorg Med Chem Lett. 2016 Feb 1;26(3):742-746. doi: 10.1016/j.bmcl.2016.01.003. Epub 2016 Jan 5. Bioorg Med Chem Lett. 2016. PMID: 26774655
Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.
Pecchi S, Renhowe PA, Taylor C, Kaufman S, Merritt H, Wiesmann M, Shoemaker KR, Knapp MS, Ornelas E, Hendrickson TF, Fantl W, Voliva CF. Pecchi S, et al. Among authors: kaufman s. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6895-8. doi: 10.1016/j.bmcl.2010.10.021. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21035331
Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.
Pecchi S, Ni ZJ, Han W, Smith A, Lan J, Burger M, Merritt H, Wiesmann M, Chan J, Kaufman S, Knapp MS, Janssen J, Huh K, Voliva CF. Pecchi S, et al. Among authors: kaufman s. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4652-6. doi: 10.1016/j.bmcl.2013.06.010. Epub 2013 Jun 12. Bioorg Med Chem Lett. 2013. PMID: 23820386
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. Among authors: kaufman s. 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.
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
Crawford TD, Romero FA, Lai KW, Tsui V, Taylor AM, de Leon Boenig G, Noland CL, Murray J, Ly J, Choo EF, Hunsaker TL, Chan EW, Merchant M, Kharbanda S, Gascoigne KE, Kaufman S, Beresini MH, Liao J, Liu W, Chen KX, Chen Z, Conery AR, Côté A, Jayaram H, Jiang Y, Kiefer JR, Kleinheinz T, Li Y, Maher J, Pardo E, Poy F, Spillane KL, Wang F, Wang J, Wei X, Xu Z, Xu Z, Yen I, Zawadzke L, Zhu X, Bellon S, Cummings R, Cochran AG, Albrecht BK, Magnuson S. Crawford TD, et al. Among authors: kaufman s. J Med Chem. 2016 Dec 8;59(23):10549-10563. doi: 10.1021/acs.jmedchem.6b01022. Epub 2016 Sep 28. J Med Chem. 2016. PMID: 27682507
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Romero FA, Murray J, Lai KW, Tsui V, Albrecht BK, An L, Beresini MH, de Leon Boenig G, Bronner SM, Chan EW, Chen KX, Chen Z, Choo EF, Clagg K, Clark K, Crawford TD, Cyr P, de Almeida Nagata D, Gascoigne KE, Grogan JL, Hatzivassiliou G, Huang W, Hunsaker TL, Kaufman S, Koenig SG, Li R, Li Y, Liang X, Liao J, Liu W, Ly J, Maher J, Masui C, Merchant M, Ran Y, Taylor AM, Wai J, Wang F, Wei X, Yu D, Zhu BY, Zhu X, Magnuson S. Romero FA, et al. Among authors: kaufman s. J Med Chem. 2017 Nov 22;60(22):9162-9183. doi: 10.1021/acs.jmedchem.7b00796. Epub 2017 Sep 21. J Med Chem. 2017. PMID: 28892380
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM. Smith A, et al. Among authors: kaufman s. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2017. PMID: 29107542
Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Lai KW, Romero FA, Tsui V, Beresini MH, de Leon Boenig G, Bronner SM, Chen K, Chen Z, Choo EF, Crawford TD, Cyr P, Kaufman S, Li Y, Liao J, Liu W, Ly J, Murray J, Shen W, Wai J, Wang F, Zhu C, Zhu X, Magnuson S. Lai KW, et al. Among authors: kaufman s. Bioorg Med Chem Lett. 2018 Jan 1;28(1):15-23. doi: 10.1016/j.bmcl.2017.11.025. Epub 2017 Nov 14. Bioorg Med Chem Lett. 2018. PMID: 29169673
1,601 results