biostudies-literatureWu GNational Natural Science Foundation of China11142-11150https://www.ebi.ac.uk/biostudies/studies/S-EPMC9063016biostudies-literatureUnknown9(20)10,11-Methylenedioxy-camptothecin (FL118) is a novel camptothecin analogue that possesses exceptional antitumor efficacy in human tumor xenograft models. The aim of the current study was to develop novel 20-substituted FL118 derivatives coupled with glycosyl-succinic acid esters with improved antitumor efficacy. These FL118 glycoside derivatives were designed, synthesized and their cytotoxicity evaluated in three tumor cell lines (A-549, MDA-MB-231 and RM-1). All of the derivatives showed superior <i>in vitro</i> cytotoxic activity and were more potent than irinotecan in A549 and MDA-MB-231 cells. In mouse prostate cancer cells RM-1, 10,11-methylenedioxy-camptothecin rhamnoside 11b displayed significant activities with IC₅₀ of 48.27 nM. Western blot analysis demonstrated that 11RSC advancesSynthesis of novel 10,11-methylenedioxy-camptothecin glycoside derivatives and investigation of their anti-tumor effects <i>in vivo</i>.PMC9063016U1406403U1706213Yu RDong XMai XXu QZhang LJiang TWu GHao CLiu FLin MfalseSynthesis of novel 10,11-methylenedioxy-camptothecin glycoside derivatives and investigation of their anti-tumor effects <i>in vivo</i>.10,11-Methylenedioxy-camptothecin (FL118) is a novel camptothecin analogue that possesses exceptional antitumor efficacy in human tumor xenograft models. The aim of the current study was to develop novel 20-substituted FL118 derivatives coupled with glycosyl-succinic acid esters with improved antitumor efficacy. These FL118 glycoside derivatives were designed, synthesized and their cytotoxicity evaluated in three tumor cell lines (A-549, MDA-MB-231 and RM-1). All of the derivatives showed superior <i>in vitro</i> cytotoxic activity and were more potent than irinotecan in A549 and MDA-MB-231 cells. In mouse prostate cancer cells RM-1, 10,11-methylenedioxy-camptothecin rhamnoside 11b displayed significant activities with IC₅₀ of 48.27 nM. Western blot analysis demonstrated that 112019-01-01T00:00:00Z2019 Apr2026-05-31T09:47:46.605Z2025-02-18T23:57:24.656ZS-EPMC90630163552022810.1039/c9ra00315k