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- Title
Rational Design of Nucleoside-Bile Acid Conjugates Incorporating a Triazole Moiety for Anticancer Evaluation and SAR Exploration.
- Authors
Navacchia, Maria Luisa; Marchesi, Elena; Mari, Lara; Chinaglia, Nicola; Gallerani, Eleonora; Gavioli, Riccardo; Capobianco, Massimo Luigi; Perrone, Daniela
- Abstract
Herein we report a study on the synthesis and biological evaluation of a library of nucleoside-bile acid conjugates prepared by combining 20-deoxyadenosine, 20-deoxyguanosine, 20-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.
- Subjects
BILE acids; NUCLEOSIDES; BILE; NUCLEOTIDES; GUANOSINE derivatives
- Publication
Molecules, 2017, Vol 22, Issue 10, p1710
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules22101710