Design, synthesis, and biological evaluation of novel nitric oxide releasing dehydroandrographolide derivatives / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
; (6): 782-790, 2018.
Article
de En
| WPRIM
| ID: wpr-812350
Bibliothèque responsable:
WPRO
ABSTRACT
A series of new hybrids of dehydroandrographolide (TAD), a biologically active natural product, bearing nitric oxide (NO)-releasing moieties were synthesized and designated as NO-donor dehydroandrographolide. The biological activities of target compounds were studied in human erythroleukemia K562 cells and breast cancer MCF-7 cells. Biological evaluation indicated that the most active compound I-5 produced high levels of NO and inhibited the proliferation of K562 (IC 1.55 μmol·L) and MCF-7 (IC 2.91 μmol·L) cells, which were more potent than the lead compound TAD and attenuated by an NO scavenger. In conclusion, I-5 is a novel hybrid with potent antitumor activity and may become a promising candidate for future intensive study.
Mots clés
Texte intégral:
1
Indice:
WPRIM
Sujet Principal:
Pharmacologie
/
Relation structure-activité
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Tests de criblage d'agents antitumoraux
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Conception de médicament
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Chimie
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Cellules K562
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Prolifération cellulaire
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Diterpènes
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Cellules MCF-7
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Antinéoplasiques
Limites du sujet:
Humans
langue:
En
Texte intégral:
Chinese Journal of Natural Medicines (English Ed.)
Année:
2018
Type:
Article