Novel derivatives of diosgenin: design, synthesis and anti-tumor activity / 药学学报
Acta Pharmaceutica Sinica
;
(12): 479-485, 2012.
Article
in Chinese
| WPRIM
| ID: wpr-323016
ABSTRACT
Diosgenin can inhibit the growth of A375 and K562 cell lines and induce their apoptosis with an effect on pro-apoptotic members of Bcl-2 family. To study the SAR of diosgenin derivatives, and to improve the anti-tumor activity of diosgenin, a series of novel diosgenin derivatives were designed and synthesized. Their anti-tumor activities in vitro were evaluated. The results revealed that most of the new derivatives had potent effects against K562, A375 and A549 (three tumor cell lines) in vitro, and had no or less effect against H293 and L02 (two normal cell lines). Particularly, some compounds (e.g. 1, 6-8) showed excellent activities on K562 with IC50 values ranging from 1.96 to 4.35 micromol x L(-1).
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Drug Design
/
Chemistry
/
Cell Line, Tumor
/
Diosgenin
/
Antineoplastic Agents
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2012
Type:
Article
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