2. Academic Validation
  3. Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation

Discovery of a photosensitizing PI3K inhibitor for tumor therapy: Design, synthesis and in vitro biological evaluation

  • Bioorg Med Chem Lett. 2023 Oct 1;94:129459. doi: 10.1016/j.bmcl.2023.129459.
Chengbin Yang 1,  Yimin Gong 2,  Mingli Deng 2,  Yun Ling 2,  Jianxin Wang 3,  Yaming Zhou 4
Affiliations

Affiliations

  • 1 Department of Pharmaceutics, School of Pharmacy, Fudan University & Key Laboratory of Smart Drug Delivery, Ministry of Education, Shanghai 201203, China; Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai 200433, China.
  • 2 Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai 200433, China.
  • 3 Department of Pharmaceutics, School of Pharmacy, Fudan University & Key Laboratory of Smart Drug Delivery, Ministry of Education, Shanghai 201203, China. Electronic address: [email protected].
  • 4 Shanghai Key Laboratory of Molecular Catalysis and Innovative Materials, Department of Chemistry, Fudan University, Shanghai 200433, China. Electronic address: [email protected].
PMID: 37634762 DOI: 10.1016/j.bmcl.2023.129459
Abstract

In drug development, optical triggering of Cancer therapy is increasingly used. Herein, we report a novel photosensitive PI3K Inhibitor FD2157, which bears a photoprotecting moiety and can be efficiently cleaved with enhanced Anticancer activity upon short-term LIGHT irradiation. In biological assessment, FD2157 exhibited remarkably enhanced Anticancer activity in inhibition of PI3K pathway against melanoma cell lines upon LIGHT irradiation (4 min). Hence, this photosensitive PI3K Inhibitor FD2157 may represent a valuable tool compound for studying the PI3K pathway and further optimization toward light-triggered Cancer treatment.

Keywords

7-azaindazole; Phosphatidylinositol 3-kinase; Photopharmacology; Photorelease; Skin cancer.

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