Design, synthesis and cytotoxicity of novel podophyllotoxin derivatives.
A series of novel podophyllotoxin derivatives were designed using association strategy and synthesized by coupling either podophyllotoxin (1) or 4beta-amino podophyllotoxin (3) with substituted indol-3-yl-glyoxyl chlorides. Their structures were identified using spectroscopic techniques. These novel derivatives have been evaluated for cytotoxicity in vitro against four human cancer cell lines with comparison to the parent compounds 1, 3 and indibulin (2). Some of the compounds (7a, 7c) showed comparable cytotoxicity to that of podophyllotoxin.
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, China.
Peng-Fei
PF
Yu
Hong
H
Chen
Jing
J
Wang
Chun-Xian
CX
He
Bo
B
Cao
Min
M
Li
Na
N
Yang
Zhi-Yong
ZY
Lei
Mao-Sheng
MS
Cheng
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003124:Colorimetry; D015195:Drug Design; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D011034:Podophyllotoxin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D012235:Rhodamines; D013778:Tetrazolium Salts; D013844:Thiazoles; D014404:Tubulin / Q000187:drug effects
D000972:Antineoplastic Agents, Phytogenic; D012235:Rhodamines; D013778:Tetrazolium Salts; D013844:Thiazoles; D014404:Tubulin; C022027:lissamine rhodamine B; C022616:thiazolyl blue; D011034:Podophyllotoxin