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Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.
Wang H, Yu N, Chen D, Lee KC, Lye PL, Chang JW, Deng W, Ng MC, Lu T, Khoo ML, Poulsen A, Sangthongpitag K, Wu X, Hu C, Goh KC, Wang X, Fang L, Goh KL, Khng HH, Goh SK, Yeo P, Liu X, Bonday Z, Wood JM, Dymock BW, Kantharaj E, Sun ET. Wang H, et al. Among authors: goh kc, goh sk, goh kl. J Med Chem. 2011 Jul 14;54(13):4694-720. doi: 10.1021/jm2003552. Epub 2011 Jun 16. J Med Chem. 2011. PMID: 21634430
SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer.
Novotny-Diermayr V, Sangthongpitag K, Hu CY, Wu X, Sausgruber N, Yeo P, Greicius G, Pettersson S, Liang AL, Loh YK, Bonday Z, Goh KC, Hentze H, Hart S, Wang H, Ethirajulu K, Wood JM. Novotny-Diermayr V, et al. Among authors: goh kc. Mol Cancer Ther. 2010 Mar;9(3):642-52. doi: 10.1158/1535-7163.MCT-09-0689. Epub 2010 Mar 2. Mol Cancer Ther. 2010. PMID: 20197387
Synthesis and evaluation of alkenyl indazoles as selective Aurora kinase inhibitors.
Blanchard S, William AD, Lee AC, Poulsen A, Teo EL, Deng W, Tu N, Tan E, Goh KL, Ong WC, Ng CP, Goh KC, Bonday Z, Sun ET. Blanchard S, et al. Among authors: goh kc, goh kl. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2443-7. doi: 10.1016/j.bmcl.2010.03.018. Epub 2010 Mar 7. Bioorg Med Chem Lett. 2010. PMID: 20338758
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma.
William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET, Goh KC, Ong WC, Goh SK, Hart S, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW. William AD, et al. Among authors: goh kc, goh sk. J Med Chem. 2011 Jul 14;54(13):4638-58. doi: 10.1021/jm200326p. Epub 2011 Jun 15. J Med Chem. 2011. PMID: 21604762
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer.
William AD, Lee AC, Goh KC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Lee CP, Wang H, Williams M, Sun ET, Hu C, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW. William AD, et al. Among authors: goh kc. J Med Chem. 2012 Jan 12;55(1):169-96. doi: 10.1021/jm201112g. Epub 2011 Dec 29. J Med Chem. 2012. PMID: 22148278
Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthritis.
William AD, Lee AC, Poulsen A, Goh KC, Madan B, Hart S, Tan E, Wang H, Nagaraj H, Chen D, Lee CP, Sun ET, Jayaraman R, Pasha MK, Ethirajulu K, Wood JM, Dymock BW. William AD, et al. Among authors: goh kc. J Med Chem. 2012 Mar 22;55(6):2623-40. doi: 10.1021/jm201454n. Epub 2012 Mar 6. J Med Chem. 2012. PMID: 22339472
2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.
Blanchard S, Soh CK, Lee CP, Poulsen A, Bonday Z, Goh KL, Goh KC, Goh MK, Pasha MK, Wang H, Williams M, Wood JM, Ethirajulu K, Dymock BW. Blanchard S, et al. Among authors: goh mk, goh kc, goh kl. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2880-4. doi: 10.1016/j.bmcl.2012.02.058. Epub 2012 Feb 27. Bioorg Med Chem Lett. 2012. PMID: 22437109
64 results