Dines, JA;
Marson, CM;
(2016)
A direct alkylation route to branched derivatives of suberoylanilide hydroxamic acid (SAHA), a potent non-selective inhibitor of histone deacetylases.
Tetrahedron
, 72
(52)
pp. 8584-8592.
10.1016/j.tet.2016.11.039.
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Abstract
Alkylation of malonamic esters provides a direct approach to derivatives of suberoylanilide hydroxamic acid (SAHA) that are branched at the amide carbon atom, a location pivotal for enhancing biological and therapeutic activity. Alkylations use NaH in THF followed by addition of the ester of 6-bromohexanoic acid; no protection of the amidic NH group is necessary. By this means, carboxylic acid, ester, amide, hydroxymethyl and 2-benzimidazolyl branching units have been appended to the SAHA backbone. Routes to vary one of the branching units at a time have been developed.
| Type: | Article |
|---|---|
| Title: | A direct alkylation route to branched derivatives of suberoylanilide hydroxamic acid (SAHA), a potent non-selective inhibitor of histone deacetylases |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1016/j.tet.2016.11.039 |
| Publisher version: | http://dx.doi.org/10.1016/j.tet.2016.11.039 |
| Language: | English |
| Additional information: | © 2016 Elsevier Ltd. All rights reserved. This manuscript version is made available under a Creative Commons Attribution Non-commercial Non-derivative 4.0 International license (CC BY-NC-ND 4.0). This license allows you to share, copy, distribute and transmit the work for personal and non-commercial use providing author and publisher attribution is clearly stated. Further details about CC BY licenses are available at https://creativecommons.org/licenses/. Access may be initially restricted by the publisher. |
| Keywords: | Malonamic esters; Alkylation; Trifunctional compounds; Suberoylanilide hydroxamic acid; Histone deacetylase inhibitors |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices UCL > Provost and Vice Provost Offices > UCL BEAMS UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences UCL > Provost and Vice Provost Offices > UCL BEAMS > Faculty of Maths and Physical Sciences > Dept of Chemistry |
| URI: | https://discovery.ucl.ac.uk/id/eprint/1533021 |
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