Synthesis and biological evaluation of novel podophyllotoxin analogs as antitumor agents.
A series of 4β N-indole-substituted podophyllotoxin derivatives were synthesized. Nine target compounds were evaluated against human cancer cell lines (HeLa, K562, and K562/A02) using MTT assay including three imine derivatives 8, 9, and 10 in vitro. The result showed that the three compounds had higher antitumor activity than their reduced forms. Among them, compounds 8, 9, 11, and 16 were superior to the positive control VP-16.
a Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics , School of Pharmacy, Tianjin Medical University , Tianjin 300070 , China.
Zhong-Heng
ZH
Zhang
Li-Ming
LM
Zhang
Gang
G
Luo
Shi
S
Zhang
Hong
H
Chen
Jing
J
Zhou
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005047:Etoposide / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D020014:K562 Cells; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D011034:Podophyllotoxin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D005047:Etoposide; D011034:Podophyllotoxin
antitumor; indole; podophyllotoxin; thiophene