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

被引：1

作者：

Yang, Chengbin ^{[1
,2
,3
]}

Gong, Yimin ^{[3
]}

Deng, Mingli ^{[3
]}

Ling, Yun ^{[3
]}

Wang, Jianxin ^{[1
,2
]}

Zhou, Yaming ^{[3
]}

机构：

[1] Fudan Univ, Sch Pharm, Dept Pharmaceut, Shanghai 201203, Peoples R China

[2] Minist Educ, Key Lab Smart Drug Delivery, Shanghai 201203, Peoples R China

[3] Fudan Univ, Dept Chem, Shanghai Key Lab Mol Catalysis & Innovat Mat, Shanghai 200433, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2023年 / 94卷

基金：

中国国家自然科学基金; 上海市自然科学基金;

关键词：

Phosphatidylinositol; 3-kinase; 7-azaindazole; Photorelease; Photopharmacology; Skin cancer; PHOTODYNAMIC THERAPY; POTENT; MALIGNANCIES; CHALLENGES; PATHWAY; CANCER; LIGHT;

D O I：

10.1016/j.bmcl.2023.129459

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页数：4

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