Glycosylation of ent-kaurene derivatives and an evaluation of their cytotoxic activities / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
; (6): 289-295, 2013.
Article
在 En
| WPRIM
| ID: wpr-812690
Responsible library:
WPRO
ABSTRACT
AIM@#To discover more active and water-soluble derivatives of tetracyclic diterpenoids containing an exo-methylene cyclopentanone or an α-methylenelactone moiety.@*METHODS@#All of the key intermediates were synthesized from stevioside, and the target compounds were obtained through glycosylation of the 4-carboxyl group. The cytotoxicity of the target compounds against six human cancer cell lines, HepG2, Bel-7402, A549, U251, MCF-7 and MDA-MB-231, were evaluated by the MTT assay.@*RESULTS@#Compound 1b was more effective than the positive control adriamycin against the HepG2, Bel-7402, A549, MCF-7, and MDA-MB-231 cell lines with IC50 values of 0.12, 0.91, 0.35, 0.08, and 0.07 μmol·L(-1), respectively. Moreover, compound 3c exhibited the most potent and selective cytotoxic activity against the HepG2 cell line (IC50, 0.01 μmol·L(-1)).@*CONCLUSION@#Compounds 1b and 3c could be considered as potential anticancer candidates for further study.
全文:
1
索引:
WPRIM
主要主题:
Glycosylation
/
Molecular Structure
/
Chemistry
/
Cell Line, Tumor
/
Diterpenes, Kaurane
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Cell Proliferation
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Drug Evaluation, Preclinical
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Toxicity
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Antineoplastic Agents
限制:
Humans
语言:
En
期刊:
Chinese Journal of Natural Medicines (English Ed.)
年:
2013
类型:
Article