title: Design and synthesis of N-phosphoryl peptide modified podophyllotoxin derivatives as potent anticancer agents.
abstract: A series of novel compounds with N-phosphoryl peptide modification at the C-4 position on podophyllotoxin were synthesized and evaluated for their cytotoxicity in vitro against K562 cell lines. Among these compounds 5c, 5f and 5k exhibited better cytotoxicity (IC(50) = 5.5 µM, 2.1 µM, and 3.1 µM, respectively) than podophyllotoxin and etoposide. Further study on compound 5f using flow cytometry analysis indicated that the anti-tumor effect might be due to the induction of apoptosis.
authors.affiliation: Key Laboratory of Chemical Biology, Guangdong Province, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055 PR China.
authors.forename: Xiangming
authors.initials: X
authors.lastname: Hu
authors.forename: Chunmei
authors.initials: C
authors.lastname: Gao
authors.forename: Chunyan
authors.initials: C
authors.lastname: Tan
authors.forename: Cunlong
authors.initials: C
authors.lastname: Zhang
authors.forename: Hualin
authors.initials: H
authors.lastname: Zhang
authors.forename: Shangfu
authors.initials: S
authors.lastname: Li
authors.forename: Hongxia
authors.initials: H
authors.lastname: Liu
authors.forename: Yuyang
authors.initials: Y
authors.lastname: Jiang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry; D011034:Podophyllotoxin / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010455:Peptides; D011034:Podophyllotoxin