Rational Design of Nucleoside-Bile Acid Conjugates Incorporating a Triazole Moiety for Anticancer Evaluation and SAR Exploration

被引：26

作者：

Navacchia, Maria Luisa ^{[1
]}

Marchesi, Elena ^{[2
]}

Mari, Lara ^{[2
]}

Chinaglia, Nicola ^{[2
]}

Gallerani, Eleonora ^{[3
]}

Gavioli, Riccardo ^{[3
]}

Capobianco, Massimo Luigi ^{[1
]}

Perrone, Daniela ^{[2
]}

机构：

[1] CNR, ISOF, Via P Gobetti 101, I-40129 Bologna, Italy

[2] Univ Ferrara, Dipartimento Sci Chim & Farmaceut, Via L Borsari 46, I-44121 Ferrara, Italy

[3] Univ Ferrara, Dipartimento Sci Vita & Biotecnol, Via L Borsari 46, I-44121 Ferrara, Italy

来源：

MOLECULES | 2017年 / 22卷 / 10期

关键词：

bioconjugates; bile acids; nucleosides; click chemistry; cytoselectivity; anticancer activity; CLICK CHEMISTRY; CANCER; TRANSPORTERS; THERAPEUTICS; ANALOGS;

D O I：

10.3390/molecules22101710

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页数：18

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