title: Synthesis and Anticancer Activity of 4β-Triazole-podophyllotoxin Glycosides.
abstract: A series of novel 4β-triazole-podophyllotoxin glycosides were synthesized by utilizing the Click reaction. Evaluation of cytotoxicity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, SW480) using MTT assay shows that most of these compounds show weak cytotoxicity. It was observed that compound 16 shows the highest activity with IC50values ranging from 2.85 to 7.28 μM, which is more potent than the control drugs etoposide and cisplatin against four of five cancer cell lines tested. Compound 16 is characterized with an α-D-galactosyl residue directly linked to the triazole ring and a 4'-OH group on the E ring of the podophyllotoxin scaffold. HPLC investigation of representative compound indicates that incorporation of a sugar moiety seems to improve the chemical stability of the podophyllotoxin scaffold.
authors: State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, 650201, China.
authors: Cheng-Ting
authors: CT
authors: Zi
authors: Gen-Tao
authors: GT
authors: Li
authors: Yan
authors: Y
authors: Li
authors: Jun
authors: J
authors: Zhou
authors: Zhong-Tao
authors: ZT
authors: Ding
authors: Zi-Hua
authors: ZH
authors: Jiang
authors: Jiang-Miao
authors: JM
authors: Hu