Synthesis and in vitro investigation of potential antiproliferative monosaccharide-d-secoestrone bioconjugates.
Bioorg Med Chem Lett
; 27(9): 1938-1942, 2017 05 01.
Article
em En
| MEDLINE
| ID: mdl-28343874
ABSTRACT
The syntheses of monosaccharide-d-secoestrone conjugates are reported. They were prepared from 3-(prop-2-inyloxy)-d-secoestrone alcohol or oxime and monosaccharide azides via Cu(I)-catalyzed azide-alkyne cycloaddition reactions (CuAAC). The antiproliferative activities of the conjugates were investigated in vitro against a panel of human adherent cancer cell lines (HeLa, A2780 and MCF-7) by means of MTT assays. The protected d-glucose-containing d-secoestrone oxime bioconjugate (24b) proved to be the most effective with an IC50 value in the low micromolar range against A2780 cell line.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Glicoconjugados
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Estrona
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Glucose
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article