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Items: 1 to 20 of 95

1.

Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.

Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB, Maciejewski P, Rossi AM, Rong H, Macaluso J, Barbosa J, Di Paolo JA, Mitchell SA.

J Med Chem. 2014 May 8;57(9):3856-73. doi: 10.1021/jm500228a. Epub 2014 Apr 29.

PMID:
24779514
2.

Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors.

Jin M, Wang J, Kleinberg A, Kadalbajoo M, Siu KW, Cooke A, Bittner MA, Yao Y, Thelemann A, Ji Q, Bhagwat S, Mulvihill KM, Rechka JA, Pachter JA, Crew AP, Epstein D, Mulvihill MJ.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):979-84. doi: 10.1016/j.bmcl.2012.12.042. Epub 2012 Dec 21.

PMID:
23317569
3.

Rational design of highly selective spleen tyrosine kinase inhibitors.

Lucas MC, Goldstein DM, Hermann JC, Kuglstatter A, Liu W, Luk KC, Padilla F, Slade M, Villaseñor AG, Wanner J, Xie W, Zhang X, Liao C.

J Med Chem. 2012 Dec 13;55(23):10414-23. doi: 10.1021/jm301367c. Epub 2012 Nov 27.

PMID:
23151054
4.

A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor.

Burke RT, Meadows S, Loriaux MM, Currie KS, Mitchell SA, Maciejewski P, Clarke AS, Dipaolo JA, Druker BJ, Lannutti BJ, Spurgeon SE.

Oncotarget. 2014 Feb 28;5(4):908-15.

5.

R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation.

Braselmann S, Taylor V, Zhao H, Wang S, Sylvain C, Baluom M, Qu K, Herlaar E, Lau A, Young C, Wong BR, Lovell S, Sun T, Park G, Argade A, Jurcevic S, Pine P, Singh R, Grossbard EB, Payan DG, Masuda ES.

J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. Epub 2006 Aug 31. Erratum in: J Pharmacol Exp Ther. 2013 May;345(2):326.

6.

Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor.

Menichincheri M, Ardini E, Magnaghi P, Avanzi N, Banfi P, Bossi R, Buffa L, Canevari G, Ceriani L, Colombo M, Corti L, Donati D, Fasolini M, Felder E, Fiorelli C, Fiorentini F, Galvani A, Isacchi A, Borgia AL, Marchionni C, Nesi M, Orrenius C, Panzeri A, Pesenti E, Rusconi L, Saccardo MB, Vanotti E, Perrone E, Orsini P.

J Med Chem. 2016 Apr 14;59(7):3392-408. doi: 10.1021/acs.jmedchem.6b00064. Epub 2016 Mar 30.

PMID:
27003761
7.

Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.

Thoma G, Veenstra S, Strang R, Blanz J, Vangrevelinghe E, Berghausen J, Lee CC, Zerwes HG.

Bioorg Med Chem Lett. 2015 Oct 15;25(20):4642-7. doi: 10.1016/j.bmcl.2015.08.037. Epub 2015 Aug 18.

PMID:
26320624
8.

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.

Pastor RM, Burch JD, Magnuson S, Ortwine DF, Chen Y, De La Torre K, Ding X, Eigenbrot C, Johnson A, Liimatta M, Liu Y, Shia S, Wang X, Wu LC, Pei Z.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2448-52. doi: 10.1016/j.bmcl.2014.04.023. Epub 2014 Apr 16.

PMID:
24767842
9.
10.

Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.

Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS, Gray M, Hayhow TG, Hobbs CI, Jones E, Leach S, Leavens K, Lewis HD, McCleary S, Neu M, Patel VK, Preston AG, Ramirez-Molina C, Shipley TJ, Skone PA, Smithers N, Somers DO, Walker AL, Watson RJ, Weingarten GG.

Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94. doi: 10.1016/j.bmcl.2011.07.082. Epub 2011 Aug 12.

PMID:
21903390
11.

Crystal structures of spleen tyrosine kinase in complex with novel inhibitors: structural insights for design of anticancer drugs.

Lee SJ, Choi JS, Han BG, Kim HS, Song HJ, Lee J, Nam S, Goh SH, Kim JH, Koh JS, Lee BI.

FEBS J. 2016 Oct;283(19):3613-3625. doi: 10.1111/febs.13831.

12.

Discovery of imidazo[1,2-b]pyridazine derivatives: selective and orally available Mps1 (TTK) kinase inhibitors exhibiting remarkable antiproliferative activity.

Kusakabe K, Ide N, Daigo Y, Itoh T, Yamamoto T, Hashizume H, Nozu K, Yoshida H, Tadano G, Tagashira S, Higashino K, Okano Y, Sato Y, Inoue M, Iguchi M, Kanazawa T, Ishioka Y, Dohi K, Kido Y, Sakamoto S, Ando S, Maeda M, Higaki M, Baba Y, Nakamura Y.

J Med Chem. 2015 Feb 26;58(4):1760-75. doi: 10.1021/jm501599u. Epub 2015 Feb 10.

PMID:
25625617
13.

Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.

Lucas MC, Bhagirath N, Chiao E, Goldstein DM, Hermann JC, Hsu PY, Kirchner S, Kennedy-Smith JJ, Kuglstatter A, Lukacs C, Menke J, Niu L, Padilla F, Peng Y, Polonchuk L, Railkar A, Slade M, Soth M, Xu D, Yadava P, Yee C, Zhou M, Liao C.

J Med Chem. 2014 Mar 27;57(6):2683-91. doi: 10.1021/jm401982j. Epub 2014 Feb 26.

PMID:
24520947
14.

Structure-activity relationship studies of imidazo[1,2-c]pyrimidine derivatives as potent and orally effective Syk family kinases inhibitors.

Hirabayashi A, Mukaiyama H, Kobayashi H, Shiohara H, Nakayama S, Ozawa M, Tsuji E, Miyazawa K, Misawa K, Ohnota H, Isaji M.

Bioorg Med Chem. 2008 Oct 15;16(20):9247-60. doi: 10.1016/j.bmc.2008.09.015. Epub 2008 Sep 9.

PMID:
18823784
15.

Discovery of new Syk inhibitors through structure-based virtual screening.

Huang Y, Zhang Y, Fan K, Dong G, Li B, Zhang W, Li J, Sheng C.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1776-1779. doi: 10.1016/j.bmcl.2017.02.060. Epub 2017 Feb 24.

PMID:
28268139
16.

Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Belanger DB, Williams MJ, Curran PJ, Mandal AK, Meng Z, Rainka MP, Yu T, Shih NY, Siddiqui MA, Liu M, Tevar S, Lee S, Liang L, Gray K, Yaremko B, Jones J, Smith EB, Prelusky DB, Basso AD.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6739-43. doi: 10.1016/j.bmcl.2010.08.140. Epub 2010 Sep 18.

PMID:
20855207
17.

Spleen tyrosine kinase inhibitors: a review of the patent literature 2010 - 2013.

Norman P.

Expert Opin Ther Pat. 2014 May;24(5):573-95. doi: 10.1517/13543776.2014.890184. Epub 2014 Feb 20. Review.

PMID:
24555683
18.

Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).

Lam B, Arikawa Y, Cramlett J, Dong Q, de Jong R, Feher V, Grimshaw CE, Farrell PJ, Hoffman ID, Jennings A, Jones B, Matuszkiewicz J, Miura J, Miyake H, Natala SR, Shi L, Takahashi M, Taylor E, Wyrick C, Yano J, Zalevsky J, Nie Z.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5947-5950. doi: 10.1016/j.bmcl.2016.10.087. Epub 2016 Nov 2.

PMID:
27839918
19.

The kinase inhibitors R406 and GS-9973 impair T cell functions and macrophage-mediated anti-tumor activity of rituximab in chronic lymphocytic leukemia patients.

Colado A, Almejún MB, Podaza E, Risnik D, Stanganelli C, Elías EE, Dos Santos P, Slavutsky I, Fernández Grecco H, Cabrejo M, Bezares RF, Giordano M, Gamberale R, Borge M.

Cancer Immunol Immunother. 2017 Apr;66(4):461-473. doi: 10.1007/s00262-016-1946-y. Epub 2016 Dec 23.

PMID:
28011996
20.

Discovery and profiling of a selective and efficacious Syk inhibitor.

Thoma G, Smith AB, van Eis MJ, Vangrevelinghe E, Blanz J, Aichholz R, Littlewood-Evans A, Lee CC, Liu H, Zerwes HG.

J Med Chem. 2015 Feb 26;58(4):1950-63. doi: 10.1021/jm5018863. Epub 2015 Feb 9.

PMID:
25633741

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