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Validation of a New Methodology to Create Oral Drugs beyond the Rule of 5 for Intracellular Tough Targets.
Ohta A, Tanada M, Shinohara S, Morita Y, Nakano K, Yamagishi Y, Takano R, Kariyuki S, Iida T, Matsuo A, Ozeki K, Emura T, Sakurai Y, Takano K, Higashida A, Kojima M, Muraoka T, Takeyama R, Kato T, Kimura K, Ogawa K, Ohara K, Tanaka S, Kikuchi Y, Hisada N, Hayashi R, Nishimura Y, Nomura K, Tachibana T, Irie M, Kawada H, Torizawa T, Murao N, Kotake T, Tanaka M, Ishikawa S, Miyake T, Tamiya M, Arai M, Chiyoda A, Akai S, Sase H, Kuramoto S, Ito T, Shiraishi T, Kojima T, Iikura H. Ohta A, et al. Among authors: emura t. J Am Chem Soc. 2023 Nov 8;145(44):24035-24051. doi: 10.1021/jacs.3c07145. Epub 2023 Oct 24. J Am Chem Soc. 2023. PMID: 37874670
Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
Kinoshita K, Ono Y, Emura T, Asoh K, Furuichi N, Ito T, Kawada H, Tanaka S, Morikami K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N. Kinoshita K, et al. Among authors: emura t. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3788-93. doi: 10.1016/j.bmcl.2011.04.020. Epub 2011 Apr 22. Bioorg Med Chem Lett. 2011. PMID: 21561771
Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist.
Nishimura Y, Esaki T, Isshiki Y, Furuta Y, Mizutani A, Kotake T, Emura T, Watanabe Y, Ohta M, Nakagawa T, Ogawa K, Arai S, Noda H, Kitamura H, Shimizu M, Tamura T, Sato H. Nishimura Y, et al. Among authors: emura t. J Med Chem. 2020 May 28;63(10):5089-5099. doi: 10.1021/acs.jmedchem.9b01743. Epub 2020 Feb 17. J Med Chem. 2020. PMID: 32022560
Development of a Scalable Synthesis of Tofogliflozin.
Ohtake Y, Emura T, Nishimoto M, Takano K, Yamamoto K, Tsuchiya S, Yeu SY, Kito Y, Kimura N, Takeda S, Tsukazaki M, Murakata M, Sato T. Ohtake Y, et al. Among authors: emura t. J Org Chem. 2016 Mar 4;81(5):2148-53. doi: 10.1021/acs.joc.5b02734. Epub 2016 Feb 19. J Org Chem. 2016. PMID: 26871504
Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
Yoshino H, Sato H, Shiraishi T, Tachibana K, Emura T, Honma A, Ishikura N, Tsunenari T, Watanabe M, Nishimoto A, Nakamura R, Nakagawa T, Ohta M, Takata N, Furumoto K, Kimura K, Kawata H. Yoshino H, et al. Among authors: emura t. Bioorg Med Chem. 2010 Dec 1;18(23):8150-7. doi: 10.1016/j.bmc.2010.10.023. Epub 2010 Oct 15. Bioorg Med Chem. 2010. PMID: 21050768
CH5137291, an androgen receptor nuclear translocation-inhibiting compound, inhibits the growth of castration-resistant prostate cancer cells.
Ishikura N, Kawata H, Nishimoto A, Nakamura R, Tsunenari T, Watanabe M, Tachibana K, Shiraishi T, Yoshino H, Honma A, Emura T, Ohta M, Nakagawa T, Houjo T, Corey E, Vessella RL, Aoki Y, Sato H. Ishikura N, et al. Among authors: emura t. Int J Oncol. 2015 Apr;46(4):1560-72. doi: 10.3892/ijo.2015.2860. Epub 2015 Jan 30. Int J Oncol. 2015. PMID: 25634071
Synthesis and optimization of hyaluronic acid-methotrexate conjugates to maximize benefit in the treatment of osteoarthritis.
Homma A, Sato H, Tamura T, Okamachi A, Emura T, Ishizawa T, Kato T, Matsuura T, Sato S, Higuchi Y, Watanabe T, Kitamura H, Asanuma K, Yamazaki T, Ikemi M, Kitagawa H, Morikawa T, Ikeya H, Maeda K, Takahashi K, Nohmi K, Izutani N, Kanda M, Suzuki R. Homma A, et al. Among authors: emura t. Bioorg Med Chem. 2010 Feb;18(3):1062-75. doi: 10.1016/j.bmc.2009.12.053. Epub 2009 Dec 28. Bioorg Med Chem. 2010. PMID: 20060728
117 results