Tisnerat, Camille, Di Ciano, Samuele, Pertusati, Fabrizio ![]() ![]() ![]() |
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License URL: http://creativecommons.org/licenses/by/4.0/
License Start date: 17 December 2024
Official URL: http://dx.doi.org/10.1021/acs.orglett.4c04379
Abstract
In this study, we report for the first time a microwave-accelerated synthesis of purine and pyrimidine nucleoside triphosphate prodrugs, whose γ phosphate is masked with an aryloxy moiety and an amino acid ester (γ-ProTriP). The synthetic utility of this method is illustrated by the synthesis of triphosphate prodrugs of clofarabine and gemcitabine, two FDA-approved anticancer drugs. These new prodrugs showed good chemical and rat serum stability. Remarkably the clofarabine prodrug showed significant cytotoxicity against a panel of cancer cell lines.
Item Type: | Article |
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Date Type: | Publication |
Status: | Published |
Schools: | Schools > Chemistry Schools > Pharmacy |
Publisher: | American Chemical Society |
ISSN: | 1523-7060 |
Funders: | MRC, Royal Society |
Date of First Compliant Deposit: | 3 January 2025 |
Date of Acceptance: | 16 December 2024 |
Last Modified: | 24 Mar 2025 16:39 |
URI: | https://orca.cardiff.ac.uk/id/eprint/174957 |
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