[S11] Developing the next generation small-molecule pharmaceuticals using a wide variety of elements

Sat. Mar 27, 2021 3:45 PM - 5:45 PM [Room D] Oral Presentation D (Online)

Organizer: Fujii Shinya (Inst. Biomaterials Bioengineering, Tokyo Med. Dent. Univ.), Ohta Kiminori (School of Pharmacy, Showa Univ.)

Drug discovery by focusing on the new chemical modalities, including antibodies, nucleic acids, cellular medicines and gene therapy, have been intensively investigated in recent years. On the other hand, the presence of low-molecular-weight (small-molecule) drugs seems to be getting smaller both in academia and in pharmaceutical companies. However, low-molecular-weight drugs have advantages in production cost and quality control, and therefore the importance of small-molecule compounds in drug discovery is not decreased. In this symposium, we will focus on the novel strategies for drug discovery with elements chemistry approaches. Though the conventional drugs consist of the common elements such as CHNOS and halogens, recently, application of various elements such as boron, silicon, and deuterium for drug discovery is coming on the limelight. Various ‘elements medicinal chemistry’ researches focusing on deuterium, boron, silicon, and arsenic, as well as the development of borofalan (¹⁰B) (Steboronine), the world’s first BNCT (boron neutron capture therapy) drug, will be presented. Development of new methodology and novel chemical modalities of small-molecules for drug discovery will be also discussed.

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オーガナイザー挨拶・趣旨説明：藤井晋也（医科歯科大生材研） (3:45 PM - 3:50 PM)

3:50 PM - 4:05 PM

[S11-1] Design strategy of biologically active compounds using a wide variety of elements

○Shinya Fujii¹ (1. Inst. Biomaterials Bioengineering, Tokyo Med. Dent. Univ.)

4:05 PM - 4:23 PM

[S11-2] Asymmetric synthesis of chiral silicon molecules and biological activity thereof

○Kazunobu Igawa¹, Katsuhiko Tomooka¹ (1. Kyushu Univ, IMCE)

4:23 PM - 4:41 PM

[S11-3] Exhaustive syntheses of deuterium-labelled compounds

○Yoshinari Sawama¹ (1. Gifu Pharmaceutical University)

4:41 PM - 4:59 PM

[S11-4] Anticancer activity of tyropeptin-boronic acid derivatives

○Isao Momose¹, Takumi Watanabe² (1. Inst. Microb. Chem. Numazu, 2. Inst. Microb. Chem.)

4:59 PM - 5:17 PM

[S11-5] Anti-tumor activity of arsenic compounds and its potential novel application in clinics

○Bo Yuan¹, Norio Takagi², Mari Okazaki¹, Toshihiko Hirano² (1. Fac. Pharm. Sci., Josai Univ., 2. Tokyo Univ of Pharm & Life Sci.)

5:17 PM - 5:40 PM

[S11-6] The new generation of particle therapy focused on boron element (boron-neutron capture therapy: BNCT) -Steboronine, the world's first approved BNCT drug-

○Hideki Nakashima¹ (1. STELLA PHARMA SakaiRDC)

まとめ：太田公規（昭和大薬） (5:40 PM - 5:45 PM)