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9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Kinoshita K, Kobayashi T, Asoh K, Furuichi N, Ito T, Kawada H, Hara S, Ohwada J, Hattori K, Miyagi T, Hong WS, Park MJ, Takanashi K, Tsukaguchi T, Sakamoto H, Tsukuda T, Oikawa N. Kinoshita K, et al. Among authors: takanashi k. J Med Chem. 2011 Sep 22;54(18):6286-94. doi: 10.1021/jm200652u. Epub 2011 Aug 25. J Med Chem. 2011. PMID: 21823617
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.
Ito T, Kinoshita K, Tomizawa M, Shinohara S, Nishii H, Matsushita M, Hattori K, Kohchi Y, Kohchi M, Hayase T, Watanabe F, Hasegawa K, Tanaka H, Kuramoto S, Takanashi K, Oikawa N. Ito T, et al. Among authors: takanashi k. J Med Chem. 2022 Sep 22;65(18):12427-12444. doi: 10.1021/acs.jmedchem.2c01099. Epub 2022 Sep 6. J Med Chem. 2022. PMID: 36066182
Selective TRK Inhibitor CH7057288 against TRK Fusion-Driven Cancer.
Tanaka H, Sase H, Tsukaguchi T, Hasegawa M, Tanimura H, Yoshida M, Sakata K, Fujii T, Tachibana Y, Takanashi K, Higashida A, Hasegawa K, Ono Y, Oikawa N, Mio T. Tanaka H, et al. Among authors: takanashi k. Mol Cancer Ther. 2018 Dec;17(12):2519-2529. doi: 10.1158/1535-7163.MCT-17-1180. Epub 2018 Sep 21. Mol Cancer Ther. 2018. PMID: 30242093
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors.
Aoki T, Hyohdoh I, Furuichi N, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ori K, Takanashi K, Harada N, Tomii Y, Tabo M, Yoshinari K, Aoki Y, Shimma N, Iikura H. Aoki T, et al. Among authors: takanashi k. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6223-7. doi: 10.1016/j.bmcl.2013.10.001. Epub 2013 Oct 9. Bioorg Med Chem Lett. 2013. PMID: 24157370
Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
Hyohdoh I, Furuichi N, Aoki T, Itezono Y, Shirai H, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ho PS, Takanashi K, Harada N, Tomii Y, Yoshinari K, Ori K, Tabo M, Aoki Y, Shimma N, Iikura H. Hyohdoh I, et al. Among authors: takanashi k. ACS Med Chem Lett. 2013 Sep 22;4(11):1059-63. doi: 10.1021/ml4002419. eCollection 2013 Nov 14. ACS Med Chem Lett. 2013. PMID: 24900605 Free PMC article.
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Aoki T, Hyohdoh I, Furuichi N, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Morikami K, Takanashi K, Harada N, Tomii Y, Shiraki K, Furumoto K, Tabo M, Yoshinari K, Ori K, Aoki Y, Shimma N, Iikura H. Aoki T, et al. Among authors: takanashi k. ACS Med Chem Lett. 2014 Jan 22;5(4):309-14. doi: 10.1021/ml400379x. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900832 Free PMC article.
214 results