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Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors. 1. Exploration of [5,6]-fused bicyclic scaffolds.
Okaniwa M, Hirose M, Imada T, Ohashi T, Hayashi Y, Miyazaki T, Arita T, Yabuki M, Kakoi K, Kato J, Takagi T, Kawamoto T, Yao S, Sumita A, Tsutsumi S, Tottori T, Oki H, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: ishikawa t. J Med Chem. 2012 Apr 12;55(7):3452-78. doi: 10.1021/jm300126x. Epub 2012 Mar 14. J Med Chem. 2012. PMID: 22376051
Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold.
Ishikawa T, Seto M, Banno H, Kawakita Y, Oorui M, Taniguchi T, Ohta Y, Tamura T, Nakayama A, Miki H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Yano J, Aertgeerts K, Kamiyama K. Ishikawa T, et al. J Med Chem. 2011 Dec 8;54(23):8030-50. doi: 10.1021/jm2008634. Epub 2011 Nov 4. J Med Chem. 2011. PMID: 22003817
Design and synthesis of pyrrolo[3,2-d]pyrimidine human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors: exploration of novel back-pocket binders.
Kawakita Y, Banno H, Ohashi T, Tamura T, Yusa T, Nakayama A, Miki H, Iwata H, Kamiguchi H, Tanaka T, Habuka N, Sogabe S, Ohta Y, Ishikawa T. Kawakita Y, et al. Among authors: ishikawa t. J Med Chem. 2012 Apr 26;55(8):3975-91. doi: 10.1021/jm300185p. Epub 2012 Apr 10. J Med Chem. 2012. PMID: 22439974
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 2. Synthesis and characterization of a novel imide-type prodrug for improving oral absorption.
Okaniwa M, Imada T, Ohashi T, Miyazaki T, Arita T, Yabuki M, Sumita A, Tsutsumi S, Higashikawa K, Takagi T, Kawamoto T, Inui Y, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: ishikawa t. Bioorg Med Chem. 2012 Aug 1;20(15):4680-92. doi: 10.1016/j.bmc.2012.06.015. Epub 2012 Jun 15. Bioorg Med Chem. 2012. PMID: 22763369
Design and synthesis of novel DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitors: 3. Evaluation of 5-amino-linked thiazolo[5,4-d]pyrimidine and thiazolo[5,4-b]pyridine derivatives.
Hirose M, Okaniwa M, Miyazaki T, Imada T, Ohashi T, Tanaka Y, Arita T, Yabuki M, Kawamoto T, Tsutsumi S, Sumita A, Takagi T, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Hirose M, et al. Among authors: ishikawa t. Bioorg Med Chem. 2012 Sep 15;20(18):5600-15. doi: 10.1016/j.bmc.2012.07.032. Epub 2012 Jul 23. Bioorg Med Chem. 2012. PMID: 22883026
Design and synthesis of potent inhibitor of apoptosis (IAP) proteins antagonists bearing an octahydropyrrolo[1,2-a]pyrazine scaffold as a novel proline mimetic.
Hashimoto K, Saito B, Miyamoto N, Oguro Y, Tomita D, Shiokawa Z, Asano M, Kakei H, Taya N, Kawasaki M, Sumi H, Yabuki M, Iwai K, Yoshida S, Yoshimatsu M, Aoyama K, Kosugi Y, Kojima T, Morishita N, Dougan DR, Snell GP, Imamura S, Ishikawa T. Hashimoto K, et al. Among authors: ishikawa t. J Med Chem. 2013 Feb 14;56(3):1228-46. doi: 10.1021/jm301674z. Epub 2013 Jan 29. J Med Chem. 2013. PMID: 23298277
Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S, Tottori T, Inui Y, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Okaniwa M, et al. Among authors: ishikawa t. J Med Chem. 2013 Aug 22;56(16):6478-94. doi: 10.1021/jm400778d. Epub 2013 Aug 1. J Med Chem. 2013. PMID: 23906342
Design, synthesis, and biological activities of novel hexahydropyrazino[1,2-a]indole derivatives as potent inhibitors of apoptosis (IAP) proteins antagonists with improved membrane permeability across MDR1 expressing cells.
Shiokawa Z, Hashimoto K, Saito B, Oguro Y, Sumi H, Yabuki M, Yoshimatsu M, Kosugi Y, Debori Y, Morishita N, Dougan DR, Snell GP, Yoshida S, Ishikawa T. Shiokawa Z, et al. Among authors: ishikawa t. Bioorg Med Chem. 2013 Dec 15;21(24):7938-54. doi: 10.1016/j.bmc.2013.09.067. Epub 2013 Oct 12. Bioorg Med Chem. 2013. PMID: 24169315
7,646 results