title: Design, synthesis, and antitumor activity of novel podophyllotoxin derivatives as potent anticancer agents.
abstract: In order to find novel synthetic compounds with superior antitumor activity and overcome multidrug resistance, a series of novel 4β-N-substituted podophyllotoxin derivatives were synthesized under mild conditions with satisfactory yield. Nine novel podophyllotoxin derivatives were synthesized by linking 4β-amino-podophyllotoxin with aldehydes via the formation of a Schiff's base, and imines were reducted to secondary amines. These novel derivatives have been evaluated for cytotoxicity against human cancer cell lines Hela, K562, and K562/AO2. The results indicated that these compounds possess superior bioactivity (IC50 values were found at the range of 10(- 6)-10(- 8) mol/l) and weak multidrug resistance.
authors.affiliation: a General Unit of Chinese People's Armed Police Force Hospital , Jiangxi Nanchang 330001 , China.
authors.forename: Jing
authors.initials: J
authors.lastname: Liu
authors.forename: Bo
authors.initials: B
authors.lastname: Cao
authors.forename: Ying
authors.initials: Y
authors.lastname: Gao
authors.forename: Mei
authors.initials: M
authors.lastname: Bai
authors.forename: Xin
authors.initials: X
authors.lastname: Mei
authors.forename: Hong
authors.initials: H
authors.lastname: Chen
authors.forename: Yun-Gen
authors.initials: YG
authors.lastname: Jiang
authors.forename: Da-Jiang
authors.initials: DJ
authors.lastname: Huang
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D018432:Drug Resistance, Multiple / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D015394:Molecular Structure; D011034:Podophyllotoxin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D011034:Podophyllotoxin