Synthesis of pyrophosphate analogues and their cytotoxic activities Article Swipe

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HeLa Phosphonate Chemistry Acridone Stereochemistry Cytotoxic T cell Pyrophosphate Alkoxy group In vitro Medicinal chemistry Organic chemistry Biochemistry Alkyl Enzyme

Van-Tai Nguyen , Phạm Minh Quân , Thi-Ha Vu , Thi-Hong-Ha Tran , Duy-Tien Doan , Dinh-Luyen Nguyen , Phong Q. Le , Van Chinh Luu ·

YOU? · · 2021 · Open Access · · DOI: https://doi.org/10.1177/17475198211043439 · OA: W3199871009

Six pyrophosphate analogues are prepared from zerumbone, murrayafoline A, acridone, and 4-hydroxycoumarin via 1,3-dipolar cycloaddition reactions. Their in vitro cytotoxic activity is evaluated against HepG2, LU-1, and HeLa cancer cell lines. Among them, diisopropyl ((ethoxy((4-((1-methoxy-3-methyl-9 H-carbazol-9-yl)methyl)-1 H-1,2,3-triazol-1-yl)methyl)phosphoryl)methyl)phosphonate (6a) and diisopropyl ((ethoxy((4-(((3-methyl-9 H-carbazol-1-yl)oxy)methyl)-1 H-1,2,3-triazol-1-yl)methyl)phosphoryl)methyl)phosphonate (6b) are found to show activity against HepG2, LU-1, and HeLa cancer cell lines, with IC 50 values ranging from 7.31 to 17.88 μM.