[Synthesis and antitumor activity of 4-alkylthio-4-deoxy-4'-demethylepipodophyllotxin derivatives].
Yao Xue Xue Bao
; 27(9): 656-61, 1992.
Article
in Zh
| MEDLINE
| ID: mdl-1293935
ABSTRACT
As a continuing part of our study on the chemistry and antitumor activity of podophyllotoxin, 11 new C-4 S-substituted podophyllotoxin derivatives were synthesised and screened in vitro against L1210 leukemia and KB cells. Thus, 4'-demethylepipodophyllotoxin was reacted with thiols in the presence of BF3. Et2O or trifluroacetic acid to give thioethers. In addition, 4-bromo-4-deoxy-4'-demethylepipodophyllotoxin, when reacted with thiols, also gave rise to corresponding thioether (4-alkylthio-4-deoxy-4'-demethylepipodophyllotoxins). Compounds 10 and 12 have the same activity as etoposide in the inhibition against L1210 leukemia, and compounds 9, 10, 12 and 15 also have comparable activity with etoposide against KB cells.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Podophyllotoxin
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
Zh
Journal:
Yao Xue Xue Bao
Year:
1992
Type:
Article