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Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents.
Kawada H, Ebiike H, Tsukazaki M, Yamamoto S, Koyama K, Nakamura M, Morikami K, Yoshinari K, Yoshida M, Ogawa K, Shimma N, Tsukuda T, Ohwada J. Kawada H, et al. Among authors: tsukazaki m. Bioorg Med Chem. 2016 Jul 1;24(13):2897-2906. doi: 10.1016/j.bmc.2016.04.060. Epub 2016 Apr 28. Bioorg Med Chem. 2016. PMID: 27189888
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: tsukazaki m. 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
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.
Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O, Kuramoto S, Ogawa K, Aoki Y, Shimma N. Ohwada J, et al. Among authors: tsukazaki m. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. doi: 10.1016/j.bmcl.2011.01.065. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316229
A water soluble prodrug of a novel camptothecin analog is efficacious against breast cancer resistance protein-expressing tumor xenografts.
Endo M, Miwa M, Ura M, Tanimura H, Taniguchi K, Miyazaki Y, Ohwada J, Tsukazaki M, Niizuma S, Murata T, Ozawa S, Suda H, Ogawa K, Nanba E, Nagao S, Shimma N, Yamada-Okabe H. Endo M, et al. Among authors: tsukazaki m. Cancer Chemother Pharmacol. 2010 Jan;65(2):363-71. doi: 10.1007/s00280-009-1042-5. Cancer Chemother Pharmacol. 2010. PMID: 19495753
15 results