Rational Design of Nucleoside-Bile Acid Conjugates Incorporating a Triazole Moiety for Anticancer Evaluation and SAR Exploration.
Molecules
; 22(10)2017 Oct 12.
Article
em En
| MEDLINE
| ID: mdl-29023408
ABSTRACT
Herein we report a study on the synthesis and biological evaluation of a library of nucleoside-bile acid conjugates prepared by combining 2'-deoxyadenosine, 2'-deoxyguanosine, 2'-deoxyuridine as well as adenosine and guanosine derivatives with cheno-, urso-, nor-cheno-, nor-urso- and taurourso-desoxycholic acid derivatives by means of the click reaction. The new nucleoside-bile acid conjugates incorporating a triazole moiety were tested in vitro against leukemic K562 and HCT116 colon carcinoma, as well as on normal fibroblast cells. Six compounds displayed interesting anti-proliferative activity against the selected cancer lines and no cytotoxic effects against normal fibroblasts. A possible structure activity relationship was also investigated.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Triazóis
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Ácidos e Sais Biliares
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Desenho de Fármacos
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Antineoplásicos
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Nucleosídeos
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article