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Asymmetric synthesis of chiral silicon molecules and biological activity thereof

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.

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

The 141st Annual Meeting of the Pharmaceutical Society of Japan (Hiroshima)

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

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