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Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors.
Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M, Sameshima T, Araki S, Endo S, Kawamoto T, Morin GB, Aparicio SA, Nakanishi A, Maezaki H, Imaeda Y. Ito M, et al. Among authors: endo s. J Med Chem. 2018 Sep 13;61(17):7710-7728. doi: 10.1021/acs.jmedchem.8b00683. Epub 2018 Aug 20. J Med Chem. 2018. PMID: 30067358
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
Miwa K, Hitaka T, Imada T, Sasaki S, Yoshimatsu M, Kusaka M, Tanaka A, Nakata D, Furuya S, Endo S, Hamamura K, Kitazaki T. Miwa K, et al. Among authors: endo s. J Med Chem. 2011 Jul 28;54(14):4998-5012. doi: 10.1021/jm200216q. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21657270
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
Kamata M, Yamashita T, Imaeda T, Tanaka T, Terauchi J, Miyamoto M, Ora T, Tawada M, Endo S, Takekawa S, Asami A, Suzuki N, Nagisa Y, Nakano Y, Watanabe K, Ogino H, Kato K, Kato K, Ishihara Y. Kamata M, et al. Among authors: endo s. Bioorg Med Chem. 2011 Sep 15;19(18):5539-52. doi: 10.1016/j.bmc.2011.07.038. Epub 2011 Jul 26. Bioorg Med Chem. 2011. PMID: 21856163
Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors.
Yamashita T, Kamata M, Endo S, Yamamoto M, Kakegawa K, Watanabe H, Miwa K, Yamano T, Funata M, Sakamoto J, Tani A, Mol CD, Zou H, Dougan DR, Sang B, Snell G, Fukatsu K. Yamashita T, et al. Among authors: endo s. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6314-8. doi: 10.1016/j.bmcl.2011.08.117. Epub 2011 Sep 6. Bioorg Med Chem Lett. 2011. PMID: 21944854
Design, synthesis, and biological evaluation of novel (1-thioxo-1,2,3,4-tetrahydro-β-carbolin-9-yl)acetic acids as selective inhibitors for AKR1B1.
Minehira D, Takeda D, Urata H, Kato A, Adachi I, Wang X, Matsuya Y, Sugimoto K, Takemura M, Endo S, Matsunaga T, Hara A, Koseki J, Narukawa K, Hirono S, Toyooka N. Minehira D, et al. Among authors: endo s. Bioorg Med Chem. 2012 Jan 1;20(1):356-67. doi: 10.1016/j.bmc.2011.10.073. Epub 2011 Nov 3. Bioorg Med Chem. 2012. PMID: 22104435
Design, synthesis and evaluation of caffeic acid phenethyl ester-based inhibitors targeting a selectivity pocket in the active site of human aldo-keto reductase 1B10.
Soda M, Hu D, Endo S, Takemura M, Li J, Wada R, Ifuku S, Zhao HT, El-Kabbani O, Ohta S, Yamamura K, Toyooka N, Hara A, Matsunaga T. Soda M, et al. Among authors: endo s. Eur J Med Chem. 2012 Feb;48:321-9. doi: 10.1016/j.ejmech.2011.12.034. Epub 2011 Dec 29. Eur J Med Chem. 2012. PMID: 22236472
Symmetrical approach of spiro-pyrazolidinediones as acetyl-CoA carboxylase inhibitors.
Kamata M, Yamashita T, Kina A, Tawada M, Endo S, Mizukami A, Sasaki M, Tani A, Nakano Y, Watanabe Y, Furuyama N, Funami M, Amano N, Fukatsu K. Kamata M, et al. Among authors: endo s. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4769-72. doi: 10.1016/j.bmcl.2012.05.062. Epub 2012 May 19. Bioorg Med Chem Lett. 2012. PMID: 22677317
2,738 results