dc.contributor.author | Welford, AJ | |
dc.contributor.author | Caldwell, JJ | |
dc.contributor.author | Liu, M | |
dc.contributor.author | Richards, M | |
dc.contributor.author | Brown, N | |
dc.contributor.author | Lomas, C | |
dc.contributor.author | Tizzard, GJ | |
dc.contributor.author | Pitak, MB | |
dc.contributor.author | Coles, SJ | |
dc.contributor.author | Eccles, SA | |
dc.contributor.author | Raynaud, FI | |
dc.contributor.author | Collins, I | |
dc.date.accessioned | 2016-08-16T15:46:11Z | |
dc.date.issued | 2016-04-11 | |
dc.identifier.citation | Chemistry (Weinheim an der Bergstrasse, Germany), 2016, 22 (16), pp. 5657 - 5664 | |
dc.identifier.issn | 0947-6539 | |
dc.identifier.uri | https://repository.icr.ac.uk/handle/internal/51 | |
dc.identifier.eissn | 1521-3765 | |
dc.identifier.doi | 10.1002/chem.201505093 | |
dc.description.abstract | The 2,11-cembranoid family of natural products has been used as inspiration for the synthesis of a structurally simplified, functionally diverse library of octahydroisobenzofuran-based compounds designed to augment a typical medicinal chemistry library screen. Ring-closing metathesis, lactonisation and SmI2 -mediated methods were exemplified and applied to the installation of a third ring to mimic the nine-membered ring of the 2,11-cembranoids. The library was assessed for aqueous solubility and permeability, with a chemical-space analysis performed for comparison to the family of cembranoid natural products and a sample set of a screening library. Preliminary investigations in cancer cells showed that the simpler scaffolds could recapitulate the reported anti-migratory activity of the natural products. | |
dc.format | Print-Electronic | |
dc.format.extent | 5657 - 5664 | |
dc.language | eng | |
dc.language.iso | eng | |
dc.publisher | WILEY-V C H VERLAG GMBH | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0 | |
dc.subject | Diterpenes | |
dc.subject | Lactones | |
dc.subject | Benzofurans | |
dc.subject | Biological Products | |
dc.subject | Chemistry, Pharmaceutical | |
dc.subject | Small Molecule Libraries | |
dc.title | Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library. | |
dc.type | Journal Article | |
dcterms.dateAccepted | 2016-04-01 | |
rioxxterms.versionofrecord | 10.1002/chem.201505093 | |
rioxxterms.licenseref.uri | https://creativecommons.org/licenses/by/4.0 | |
rioxxterms.licenseref.startdate | 2016-04 | |
rioxxterms.type | Journal Article/Review | |
dc.relation.isPartOf | Chemistry (Weinheim an der Bergstrasse, Germany) | |
pubs.issue | 16 | |
pubs.notes | No embargo | |
pubs.organisational-group | /ICR | |
pubs.organisational-group | /ICR/Primary Group | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 1 | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 2 | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 4 (including Analytical Chemistry) | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Tumour Biology & Metastasis | |
pubs.organisational-group | /ICR | |
pubs.organisational-group | /ICR/Primary Group | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 1 | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 2 | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 4 (including Analytical Chemistry) | |
pubs.organisational-group | /ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Tumour Biology & Metastasis | |
pubs.publication-status | Published | |
pubs.volume | 22 | |
pubs.embargo.terms | No embargo | |
icr.researchteam | Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
icr.researchteam | Medicinal Chemistry 1 | |
icr.researchteam | Medicinal Chemistry 2 | |
icr.researchteam | Medicinal Chemistry 4 (including Analytical Chemistry) | |
icr.researchteam | Tumour Biology & Metastasis | |
dc.contributor.icrauthor | Caldwell, John | |
dc.contributor.icrauthor | Liu, Manjuan | |
dc.contributor.icrauthor | Richards, Gareth | |
dc.contributor.icrauthor | Eccles, Suzanne | |
dc.contributor.icrauthor | Raynaud, Florence | |
dc.contributor.icrauthor | Collins, Ian | |