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Page 1
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: rix p. J Med Chem. 2009 May 14;52(9):3047-62. doi: 10.1021/jm900173b. J Med Chem. 2009. PMID: 19374401
Pharmacological characterization of KLYP961, a dual inhibitor of inducible and neuronal nitric-oxide synthases.
Symons KT, Nguyen PM, Massari ME, Anzola JV, Staszewski LM, Wang L, Yazdani N, Dorow S, Muhammad J, Sablad M, Rozenkrants N, Bonefous C, Payne JE, Rix PJ, Shiau AK, Noble SA, Smith ND, Hassig CA, Zhang Y, Rao TS. Symons KT, et al. J Pharmacol Exp Ther. 2011 Feb;336(2):468-78. doi: 10.1124/jpet.110.172817. Epub 2010 Oct 29. J Pharmacol Exp Ther. 2011. PMID: 21036913
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: rix p. 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: rix p. J Med Chem. 2010 Nov 11;53(21):7739-55. doi: 10.1021/jm100828n. J Med Chem. 2010. PMID: 20931971
Heteroaromatic-aminomethyl quinolones: potent and selective iNOS inhibitors.
Durón SG, Lindstrom A, Bonnefous C, Zhang H, Chen X, Symons KT, Sablad M, Rozenkrants N, Zhang Y, Wang L, Yazdani N, Shiau AK, Noble SA, Rix P, Rao TS, Hassig CA, Smith ND. Durón SG, et al. Among authors: rix p. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1237-41. doi: 10.1016/j.bmcl.2011.11.073. Epub 2011 Nov 25. Bioorg Med Chem Lett. 2012. PMID: 22182498
Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Lai A, Kahraman M, Govek S, Nagasawa J, Bonnefous C, Julien J, Douglas K, Sensintaffar J, Lu N, Lee KJ, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Moon MJ, Joseph JD, Darimont B, Brigham D, Grillot K, Heyman R, Rix PJ, Hager JH, Smith ND. Lai A, et al. Among authors: rix pj. J Med Chem. 2015 Jun 25;58(12):4888-904. doi: 10.1021/acs.jmedchem.5b00054. Epub 2015 May 22. J Med Chem. 2015. PMID: 25879485
Optimization of an indazole series of selective estrogen receptor degraders: Tumor regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Nagasawa JY, Douglas KL, Lai AG, Kahraman M, Bonnefous C, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND. Govek SP, et al. Among authors: rix pj. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5163-7. doi: 10.1016/j.bmcl.2015.09.074. Epub 2015 Oct 3. Bioorg Med Chem Lett. 2015. PMID: 26463130
Maximizing ER-α Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.
Kahraman M, Govek SP, Nagasawa JY, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Liu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Heyman R, Rix PJ, Hager JH, Smith ND. Kahraman M, et al. Among authors: rix pj. ACS Med Chem Lett. 2018 Dec 6;10(1):50-55. doi: 10.1021/acsmedchemlett.8b00414. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655946 Free PMC article.
Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.
Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Lu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Maheu K, Heyman R, Rix PJ, Hager JH, Smith ND. Nagasawa J, et al. Among authors: rix pj. J Med Chem. 2018 Sep 13;61(17):7917-7928. doi: 10.1021/acs.jmedchem.8b00921. Epub 2018 Sep 4. J Med Chem. 2018. PMID: 30086626
Selective estrogen receptor degraders with novel structural motifs induce regression in a tamoxifen-resistant breast cancer xenograft.
Govek SP, Bonnefous C, Julien JD, Nagasawa JY, Kahraman M, Lai AG, Douglas KL, Aparicio AM, Darimont BD, Grillot KL, Joseph JD, Kaufman JA, Lee KJ, Lu N, Moon MJ, Prudente RY, Sensintaffar J, Rix PJ, Hager JH, Smith ND. Govek SP, et al. Among authors: rix pj. Bioorg Med Chem Lett. 2019 Feb 1;29(3):367-372. doi: 10.1016/j.bmcl.2018.12.042. Epub 2018 Dec 19. Bioorg Med Chem Lett. 2019. PMID: 30587451
35 results