Author/Authors :
Wu، نويسنده , , Yuelin and Zhu، نويسنده , , Lingjian and Sheng، نويسنده , , Chunquan and Yao، نويسنده , , Jianzhong and Miao، نويسنده , , Zhenyuan and Zhang، نويسنده , , Wannian and Wei، نويسنده , , Yunyang and Shi، نويسنده , , Ruofu، نويسنده ,
Abstract :
It is an important strategy for fluorine substitution in drug design because of its small size and high electronegativity. Fluorinated 10-hydroxycamptothecin and SN 38 were prepared and screened for antiproliferative activities. Among them, fluorinated compound MF-6 showed higher antiproliferative activities against A549, HCT116 and MDA-MB-435 cancer cells than unfluorinated compound. The result of Topoisomerase I activity also confirmed that the C-21 carbonyl group of camptothecin structure is unnecessary to antitumor activity.
