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New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation

New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation
New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation
New synthetic routes towards the natural product psammaplin A were developed with the particular view to preparing diverse analogues for biological assessment. These routes utilize cheap and commercially available starting materials, and allowed access to psammaplin A analogues not accessible via currently reported methods. Preliminary biological studies revealed these compounds to be the most potent non peptidic inhibitors of the enzyme histone deacetylase 1 (HDAC1, class I) discovered so far. Interestingly, psammaplin A and our synthetic analogues show class I selectivity in vitro, an important feature for the design and synthesis of future isoform selective inhibitors.
1477-0520
659-662
Baud, Matthias
8752d519-3d33-43b6-9a77-ab731d410c2e
Leiser, Thomas
0a989c0c-4a10-4fb3-95eb-e7f511229e14
Meyer-Almes, Franz-Josef
9f252633-80d9-4a9b-bcc7-96c0891a2dcf
Fuchter, Matthew J.
a98083c4-2a98-4844-8289-5468ec472801
Baud, Matthias
8752d519-3d33-43b6-9a77-ab731d410c2e
Leiser, Thomas
0a989c0c-4a10-4fb3-95eb-e7f511229e14
Meyer-Almes, Franz-Josef
9f252633-80d9-4a9b-bcc7-96c0891a2dcf
Fuchter, Matthew J.
a98083c4-2a98-4844-8289-5468ec472801

Baud, Matthias, Leiser, Thomas, Meyer-Almes, Franz-Josef and Fuchter, Matthew J. (2011) New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation. Organic & Biomolecular Chemistry, 9 (3), 659-662. (doi:10.1039/C0OB00824A).

Record type: Article

Abstract

New synthetic routes towards the natural product psammaplin A were developed with the particular view to preparing diverse analogues for biological assessment. These routes utilize cheap and commercially available starting materials, and allowed access to psammaplin A analogues not accessible via currently reported methods. Preliminary biological studies revealed these compounds to be the most potent non peptidic inhibitors of the enzyme histone deacetylase 1 (HDAC1, class I) discovered so far. Interestingly, psammaplin A and our synthetic analogues show class I selectivity in vitro, an important feature for the design and synthesis of future isoform selective inhibitors.

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More information

e-pub ahead of print date: 12 November 2010
Published date: 2011

Identifiers

Local EPrints ID: 400517
URI: https://eprints.soton.ac.uk/id/eprint/400517
ISSN: 1477-0520
PURE UUID: 5f91f2ed-e929-4bce-af66-ae33afebf8ef
ORCID for Matthias Baud: ORCID iD orcid.org/0000-0003-3714-4350

Catalogue record

Date deposited: 21 Sep 2016 15:29
Last modified: 14 Jul 2018 00:28

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