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Molecules 2017, 22(10), 1710; doi:10.3390/molecules22101710

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

1
Consiglio Nazionale delle Ricerche, Istituto per la Sintesi Organica e la Fotoreattività (CNR-ISOF), via P. Gobetti 101, 40129 Bologna, Italy
2
Dipartimento di Scienze Chimiche e Farmaceutiche, Università degli studi di Ferrara, via L. Borsari 46, 44121 Ferrara, Italy
3
Dipartimento di Scienze della Vita e Biotecnologie, Università degli studi di Ferrara, via L. Borsari 46, 44121 Ferrara, Italy
*
Author to whom correspondence should be addressed.
Received: 27 September 2017 / Revised: 9 October 2017 / Accepted: 10 October 2017 / Published: 12 October 2017
(This article belongs to the Special Issue Medicinal Chemistry in Europe)
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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. View Full-Text
Keywords: bioconjugates; bile acids; nucleosides; click chemistry; cytoselectivity; anticancer activity bioconjugates; bile acids; nucleosides; click chemistry; cytoselectivity; anticancer activity
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Navacchia, M.L.; Marchesi, E.; Mari, L.; Chinaglia, N.; Gallerani, E.; Gavioli, R.; Capobianco, M.L.; Perrone, D. Rational Design of Nucleoside–Bile Acid Conjugates Incorporating a Triazole Moiety for Anticancer Evaluation and SAR Exploration. Molecules 2017, 22, 1710.

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