Synthesis and antitumor activity of S-hexyl(heptyl) substituted ethanethioate derivatives / 药学学报
Acta Pharmaceutica Sinica
; (12): 352-358, 2014.
Article
de Zh
| WPRIM
| ID: wpr-245078
Bibliothèque responsable:
WPRO
ABSTRACT
To simplify the macrocyclic fragment and to modify the zinc binding group of the natural product apicidin, two series of S-hexyl (heptyl) ethanethioate derivatives were designed and synthesized. Twenty-six compounds were synthesized and confirmed with 1H NMR, IR, MS and HR-MS spectrum, which were not reported. Take vorinostat as control, their antiporliferative activities against cancer cell lines, MCF-7 and HL-60, were tested with MTT assay or trypan blue staining method. Generally in both series it was found that, the chiral carbon atom at 7 position is not necessary, compounds II-1, II-3, II-6 and II-13 showed good activity on HL-60 cells in vitro, with the IC50 values less than 10 micromol x L(-1). II-7 and II-8 showed stronger activity against MCF-7 than Vorinostat, with the IC50 of 3.19 and 6.29 micromol x L(-1), respectively.
Texte intégral:
1
Indice:
WPRIM
Sujet Principal:
Peptides cycliques
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Pharmacologie
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Relation structure-activité
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Tests de criblage d'agents antitumoraux
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Chimie
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Cellules HL-60
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Concentration inhibitrice 50
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Prolifération cellulaire
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Inhibiteurs de désacétylase d'histone
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Cellules MCF-7
Limites du sujet:
Humans
langue:
Zh
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2014
Type:
Article