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

Chengbin Yang,Yimin Gong,Mingli Deng,Yun Ling,Jianxin Wang,Yaming Zhou

Bioorganic & medicinal chemistry letters（2023）

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摘要

•A 7-azaindazole derivative, FD2157, was designed and synthesized as a photosensitizing PI3K inhibitor.•FD2157 showed excellent in vitro anti-melanoma cell activity under UV light activation.•FD2157 could significantly induce apoptosis upon UV light irradiation and arrest the cell cycle at the G2/M phase in B16 cells.

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关键词

Phosphatidylinositol 3-kinase,7-azaindazole,Photorelease,Photopharmacology,Skin cancer

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