Gifu, Japan

Pharmaceutical and Medicinal Chemistry

Research Interests

We are working on understanding the living systems and challenging diseases based on principles and technology of organic chemistry. One of the key aims of our research is cancer drug development through a chemical biological approach for cancer research. Especially, by focusing on tumor microenvironment characterized by hypoxia and low nutrition “microenvironment modulators” such as angiogenesis inhibitor and anti-austerity agents have been developed as novel cytostatic cancer agents. For development of non-invasive cancer diagnostic technique, novel NIR-fluorescent probes are produced for visualizing hypoxic region. As a chemical tool to study biological processes, we are creating unique fluorescent probes for labile divalent iron. Disorders of iron homeostasis associate with the oxidative stress conditions and refractory diseases such as cancer and neurodegeneration. Furthermore, we are developing useful reactions for drug development such as various catalytic C-H functionalization reactions and oxidative coupling reactions, and a practical synthetic procedure of macrocyclic scaffolds in medicinal chemistry. (URL:

Research Objectives
  1. Anticancer drug development targeting the tumor microenvironment and cancer chemical biology
  2. Development of novel chemical tools to study diseases and biological processes
  3. Development of fluorescent probes for elucidation of iron homeostasis
  4. Development of diversity-oriented synthesis for drug discovery
Research Results
  1. Hattori K., Koike K., Okuda K., Hirayama T., Ebihara M., Takenaka M., Nagasawa H., Solution-phase synthesis and biological evaluation of triostin A and its analogues., Org. Biomol. Chem., 14, 2090-2111(2016).
  2. Niwa M., Hirayama T., Okuda K., Nagasawa H., A new class of high-contrast Fe(II) selective fluorescent probes based on spirocyclized scaffolds for visualization of intracellular labile iron delivered by transferrin., Org. Biomol.Chem., 12, 6590-6597(2014).
  3. Narise K., Okuda K., Enomoto Y., Hirayama T., Nagasawa H., Optimization of biguanide derivatives as selective antitumor agents blocking adaptive stress responses in the tumor microenvironment, Drug Des. Devel. Ther., 2014(8),701–717 (2014).
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