|organic synthetic chemistry，drug discovery science，kinase inhibitor|
Education and Research Activities in the Laboratory
We foster human resources who have the ability to find and solve research challenges, as well as those who can contribute to society through research activities on drug discovery based on synthetic organic chemistry. We provide research and education, aiming to foster human resources who dream of performing skilled manufacturing and spare no effort in achieving the dream. Thus, we place emphasis on the understanding of research background and positioning, experimental design and techniques, result analysis, discussion, and how to derive conclusions. We provide guidance to students so that they can acquire the basic experimental capability to obtain correct and reliable data and, at the same time, give consideration to safety and health during actual chemical experiments.
The Functional Polymer Science Laboratory, a collaboration course between Santen Pharmaceutical Co., Ltd. and Nara Institute of Science and Technology, has been conducting research activity since April 2005. Our main research themes are basic synthetic organic chemistry for drug discovery and search for candidate compounds for developing new medicinal drugs with unique structures. In particular, we are synthesizing and conducting the functional evaluation (screening) of compounds that can inhibit protein kinase, a target of molecularly targeted agents recently attracting increasing attention in various fields. For compound synthesis, we use the reaction of TFP-resin in its solid-phase to study parallel synthesis (1,4-benzoxazin-3-one derivatives) (Fig. 1), whereas for drug design, we search for compounds that can secure a three-dimensional stable conformation suitable for active expression when they feature intramolecular nonbonded interaction (nonbonded interaction between hetero atoms such as hydrogen bond, N, O, and S).
Explanatory Pictures of Research Activities
Fig. 1 Resin-based solid-phase synthesis
Fig. 2 Compounds with kinase-inhibition activity based on intramolecular nonbonded interaction
Recent Research Papers and Achievements
Academic conference presentation
The 25th Medicinal Chemistry Symposium 2006 (Nagoya) (in Japanese)
The 26th Medicinal Chemistry Symposium 2007 (Sagami-Ohno) (in Japanese)
The 27th Medicinal Chemistry Symposium 2008 (Osaka) (in Japanese)
The 29th Medicinal Chemistry Symposium 2010 (Kyoto) (in Japanese)
The 127th Annual Meeting of the Pharmaceutical Society of Japan 2007 (Toyama) (in Japanese)
The 128th Annual Meeting of the Pharmaceutical Society of Japan 2008 (Yokohama) (in Japanese)
The 129th Annual Meeting of the Pharmaceutical Society of Japan 2009 (Okayama) (in Japanese)
The 37th Symposium on Heterocyclic Chemistry 2007 (Nagano) (in Japanese)
The 38th Symposium on Heterocyclic Chemistry 2008 (Fukuyama) (in Japanese)
The 39th Symposium on Heterocyclic Chemistry 2009 (Kashiwa) (in Japanese)
ISIS5 2008 (Kobe) (in English)
T. Honda, et al. Bioorg. Med. Chem. Lett. 18, 2939 (2008).
T. Honda, et al. Bioorg. Med. Chem. 17, 699 (2009).
H. Tajima, et al. Bioorg. Med. Chem. Lett. 20, 7234 (2010).
T. Honda, et al. Bioorg. Med. Chem. Lett. 21, 1782 (2011).
H. Tajima, et al. Bioorg. Med. Chem. Lett. 21, 1232 (2011).