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Page 1
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.
Pinkerton AB, Lee TT, Hoffman TZ, Wang Y, Kahraman M, Cook TG, Severance D, Gahman TC, Noble SA, Shiau AK, Davis RL. Pinkerton AB, et al. Among authors: shiau ak. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3562-9. doi: 10.1016/j.bmcl.2007.04.076. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17498954
KD5170, a novel mercaptoketone-based histone deacetylase inhibitor that exhibits broad spectrum antitumor activity in vitro and in vivo.
Hassig CA, Symons KT, Guo X, Nguyen PM, Annable T, Wash PL, Payne JE, Jenkins DA, Bonnefous C, Trotter C, Wang Y, Anzola JV, Milkova EL, Hoffman TZ, Dozier SJ, Wiley BM, Saven A, Malecha JW, Davis RL, Muhammad J, Shiau AK, Noble SA, Rao TS, Smith ND, Hager JH. Hassig CA, et al. Among authors: shiau ak. Mol Cancer Ther. 2008 May;7(5):1054-65. doi: 10.1158/1535-7163.MCT-07-2347. Mol Cancer Ther. 2008. PMID: 18483295
Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.
Payne JE, Bonnefous C, Hassig CA, Symons KT, Guo X, Nguyen PM, Annable T, Wash PL, Hoffman TZ, Rao TS, Shiau AK, Malecha JW, Noble SA, Hager JH, Smith ND. Payne JE, et al. Among authors: shiau ak. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6093-6. doi: 10.1016/j.bmcl.2008.10.029. Epub 2008 Oct 11. Bioorg Med Chem Lett. 2008. PMID: 18954983
Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models.
Bonnefous C, Payne JE, Roppe J, Zhuang H, Chen X, Symons KT, Nguyen PM, Sablad M, Rozenkrants N, Zhang Y, Wang L, Severance D, Walsh JP, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND. Bonnefous C, et al. Among authors: shiau ak. J Med Chem. 2009 May 14;52(9):3047-62. doi: 10.1021/jm900173b. J Med Chem. 2009. PMID: 19374401
Water-soluble PDE4 inhibitors for the treatment of dry eye.
Govek SP, Oshiro G, Anzola JV, Beauregard C, Chen J, Coyle AR, Gamache DA, Hellberg MR, Hsien JN, Lerch JM, Liao JC, Malecha JW, Staszewski LM, Thomas DJ, Yanni JM, Noble SA, Shiau AK. Govek SP, et al. Among authors: shiau ak. Bioorg Med Chem Lett. 2010 May 1;20(9):2928-32. doi: 10.1016/j.bmcl.2010.03.023. Epub 2010 Mar 7. Bioorg Med Chem Lett. 2010. PMID: 20378348
Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.
Davis RL, Kahraman M, Prins TJ, Beaver Y, Cook TG, Cramp J, Cayanan CS, Gardiner EM, McLaughlin MA, Clark AF, Hellberg MR, Shiau AK, Noble SA, Borchardt AJ. Davis RL, et al. Among authors: shiau ak. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3361-6. doi: 10.1016/j.bmcl.2010.04.020. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20434334
Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
Herbert MR, Siegel DL, Staszewski L, Cayanan C, Banerjee U, Dhamija S, Anderson J, Fan A, Wang L, Rix P, Shiau AK, Rao TS, Noble SA, Heyman RA, Bischoff E, Guha M, Kabakibi A, Pinkerton AB. Herbert MR, et al. Among authors: shiau ak. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21. doi: 10.1016/j.bmcl.2010.08.014. Epub 2010 Aug 10. Bioorg Med Chem Lett. 2010. PMID: 20801037
Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNOS dimerization inhibitors that are orally active in pain models.
Payne JE, Bonnefous C, Symons KT, Nguyen PM, Sablad M, Rozenkrants N, Zhang Y, Wang L, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND. Payne JE, et al. Among authors: shiau ak. J Med Chem. 2010 Nov 11;53(21):7739-55. doi: 10.1021/jm100828n. J Med Chem. 2010. PMID: 20931971
65 results