title: Synthesis and cytotoxic activity of novel derivatives of 4'-demethylepipodophyllotoxin.
abstract: Nine novel 4beta-N-substituted-5-FU-4'-demethylepipodophyllotoxin derivatives were synthesized and evaluated as potential antitumor agents. All of the target compounds showed more significant cytotoxic activity against HL-60 and A-549 in vitro than VP-16 and 5-FU. Among them, 4beta-N-substituted-phenylalanine 5-Fu pentyl ester-4'-demethylepipodophyllotoxin (9 g) was found to exhibit most potent cytotoxic activity against HL-60 and A-549 cell (IC50 is 0.04 and <0.01 microM, respectively).
authors.affiliation: State Key Laboratory of Applied Organic Chemistry and Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
authors.forename: Shi-Wu
authors.initials: SW
authors.lastname: Chen
authors.forename: Xuan
authors.initials: X
authors.lastname: Tian
authors.forename: Yong-Qiang
authors.initials: YQ
authors.lastname: Tu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005047:Etoposide / Q000494:pharmacology; D005472:Fluorouracil / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D011034:Podophyllotoxin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D005047:Etoposide; D011034:Podophyllotoxin; D005472:Fluorouracil; C072088:4'-demethylepipodophyllotoxin