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.

Rational design of nucleoside-bile acid conjugates incorporating a triazole moiety for anticancer evaluation and SAR exploration

Elena Marchesi
Secondo
;
Lara Mari;Nicola Chinaglia;Eleonora Gallerani;Riccardo Gavioli;Daniela Perrone
Ultimo
2017

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.
Luisa Navacchia, Maria; Marchesi, Elena; Mari, Lara; Chinaglia, Nicola; Gallerani, Eleonora; Gavioli, Riccardo; Luigi Capobianco, Massimo; Perrone, Daniela
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2382160
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