[Synthesis and antitumor activity of 4-S-(5-amido-1,3,4-thiodiazol-2-yl)4-deoxy-4'-demethylepipodophyllotoxi n analogues].
By the condensation of 4'-demethylepipodophyllotoxin with 2-amino-5-mercapto-1,3,4-thiodiazole in CF3COOH and acylation in the presence of DEPC, 10 title compounds were conveniently synthesized. These compounds were screened in vitro against L1210 leukemia and KB cells, in which compounds SIPI-92-1772, 1774, 1775, 1776, 1777 and 1779 exhibited more potent anti-tumor activity.
Yin
S F
SF
Shanghai Institute of Pharmaceutical Industry.
Zhuang
W
W
Ma
W Y
WY
Wang
Z G
ZG
Wang
T D
TD
Chen
X H
XH
Zhang
C N
CN
D000818:Animals; D005047:Etoposide / Q000494:pharmacology; D006801:Humans; D007624:KB Cells / Q000187:drug effects; D007939:Leukemia L1210 / Q000473:pathology; D011034:Podophyllotoxin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D005047:Etoposide; D011034:Podophyllotoxin