| Literature DB >> 20363623 |
Joachim Caron1, L Harivardhan Reddy, Sinda Lepêtre-Mouelhi, Séverine Wack, Pascal Clayette, Christine Rogez-Kreuz, Rahima Yousfi, Patrick Couvreur, Didier Desmaële.
Abstract
4-(N)-1,1',2-trisnor-squalenoyldideoxycytidine monophosphate (SQddC-MP) and 4-(N)-1,1',2-trisnor-squalenoylgemcitabine monophosphate (SQdFdC-MP) were synthesized using phosphoramidite chemistry. These amphiphilic molecules self-assembled to about hundred nanometers size nanoassemblies in aqueous medium. Nanoassemblies of SQddC-MP displayed significant anti-HIV activity whereas SQdFdC-MP nanoassemblies displayed promising anticancer activity on leukemia cells. These results suggested that squalene conjugate of negatively charged nucleotide analogues efficiently penetrated within cells. Thus, we propose a new prodrug strategy for improved delivery of nucleoside analogues to ameliorate their biological efficacy. 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20363623 DOI： 10.1016/j.bmcl.2010.03.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823