ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites

ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites

•Synthesis of 46 BVdU ProTide derivatives with superior activity over BVdU.•Anti-proliferative activity against L1210, CEM, HeLa and HEL cell lines.•Up to 20-fold cytostatic activity enhancement over the parent BVdU.•Retention or increase of the cytostatic activity against TK-deficient cancer cells....

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Main Authors: Kandil, Sahar, Balzarini, Jan, Rat, Stephanie, Brancale, Andrea, Westwell, Andrew D., McGuigan, Christopher
Format: Online
Language:English
Published: Elsevier Science Ltd 2016
Online Access:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5131913/
id pubmed-5131913
recordtype oai_dc
spelling pubmed-51319132016-12-06 ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites Kandil, Sahar Balzarini, Jan Rat, Stephanie Brancale, Andrea Westwell, Andrew D. McGuigan, Christopher Article •Synthesis of 46 BVdU ProTide derivatives with superior activity over BVdU.•Anti-proliferative activity against L1210, CEM, HeLa and HEL cell lines.•Up to 20-fold cytostatic activity enhancement over the parent BVdU.•Retention or increase of the cytostatic activity against TK-deficient cancer cells.•Separation of 4 pairs of P diastereoisomers and comparison of their properties. Elsevier Science Ltd 2016-12-01 /pmc/articles/PMC5131913/ /pubmed/27818111 http://dx.doi.org/10.1016/j.bmcl.2016.10.077 Text en © 2016 The Authors http://creativecommons.org/licenses/by/4.0/ This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).
repository_type Open Access Journal
institution_category Foreign Institution
institution US National Center for Biotechnology Information
building NCBI PubMed
collection Online Access
language English
format Online
author Kandil, Sahar
Balzarini, Jan
Rat, Stephanie
Brancale, Andrea
Westwell, Andrew D.
McGuigan, Christopher
spellingShingle Kandil, Sahar
Balzarini, Jan
Rat, Stephanie
Brancale, Andrea
Westwell, Andrew D.
McGuigan, Christopher
ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
author_facet Kandil, Sahar
Balzarini, Jan
Rat, Stephanie
Brancale, Andrea
Westwell, Andrew D.
McGuigan, Christopher
author_sort Kandil, Sahar
title ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
title_short ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
title_full ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
title_fullStr ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
title_full_unstemmed ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
title_sort protides of bvdu as potential anticancer agents upon efficient intracellular delivery of their activated metabolites
description •Synthesis of 46 BVdU ProTide derivatives with superior activity over BVdU.•Anti-proliferative activity against L1210, CEM, HeLa and HEL cell lines.•Up to 20-fold cytostatic activity enhancement over the parent BVdU.•Retention or increase of the cytostatic activity against TK-deficient cancer cells.•Separation of 4 pairs of P diastereoisomers and comparison of their properties.
publisher Elsevier Science Ltd
publishDate 2016
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5131913/
_version_ 1613750300206694400

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