(SD2021-146) ANTICANCER AND ANTIFUNGAL SPLICE MODULATORS

Tech ID: 32495 / UC Case 2021-Z08-1

Background

While splice modulators have entered clinical trials, limited clinical efficacy in splicing factor mutation-driven malignancies, such as acute myeloid leukemia, has remained a challenge. There is a pressing unmet medical need for developing potent small molecule splice modulators for the treatment of a broad array of malignancies characterized by splicing deregulation. 

However, the inability to practically access gram-scale lead molecules with viable pharmacological properties continues to hinder their application.

Technology Description

Researchers from UC San Diego report on a scalable approach to prepare 17S-FD-895, a potent in vivo active splice modulator. The strategy described herein not only provides material to enable clinical translation but also furthers lead validation by expanding the structure-activity relationships that guide splice modulation.

Advantages

  • Process scaled synthesis of a complex polyketide
  • Complete control of regioselective bond assembly
  • Installation of 11 stereocenters with high enantioselectivity
  • Synthetic access to single stereoisomeric and single-atom isotopically labeled analogs

State Of Development

Intellectual Property Info

UC San Diego is seeking companies interested in commercializing this technology into products.

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Other Information

Keywords

medicinal chemistry, polyketide, stereochemistry, splicing modulator, process chemistry

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