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All Outputs (5)

Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery (2017)
Journal Article
Geary, G. C., Nortcliffe, A., Pearce, C. A., Hamza, D., Jones, G., & Moody, C. J. (in press). Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery. Bioorganic and Medicinal Chemistry, https://doi.org/10.1016/j.bmc.2017.12.012

A spirocyclic, sp3-atom rich oxetane-containing scaffold was synthesised in just two steps via a gold catalysed propargylic alcohol rearrangement. The key gold cyclisation can be undertaken on a 40 g scale allowing the preparation of 419 lead-like co... Read More about Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery.

Development of a series of bis-triazoles as G-quadruplex ligands (2017)
Journal Article
Saleh, M., Laughton, C. A., Bradshaw, T. D., & Moody, C. J. (in press). Development of a series of bis-triazoles as G-quadruplex ligands. RSC Advances, 7, https://doi.org/10.1039/c7ra07257k

Maintenance of telomeres – specialized complexes that protect the ends of chromosomes – is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells. Targeting... Read More about Development of a series of bis-triazoles as G-quadruplex ligands.

C–H insertion as a key step to spiro-oxetanes, scaffolds for drug discovery (2017)
Journal Article
Nicolle, S. M., Nortcliffe, A., Bartrum, H. E., Lewis, W., Hayes, C. J., & Moody, C. J. (in press). C–H insertion as a key step to spiro-oxetanes, scaffolds for drug discovery. Chemistry - A European Journal, https://doi.org/10.1002/chem.201703746

A new route to spiro-oxetanes, potential scaffolds for drug discovery, is described. The route is based on the selective 1,4-C–H insertion reactions of metallocarbenes, generated from simple carbonyl precursors in flow or batch mode, to give spiro-β-... Read More about C–H insertion as a key step to spiro-oxetanes, scaffolds for drug discovery.

Total synthesis of the cyclic dodecapeptides wewakazole and wewakazole B (2017)
Journal Article
Inman, M., Dexter, H. L., & Moody, C. J. (2017). Total synthesis of the cyclic dodecapeptides wewakazole and wewakazole B. Organic Letters, 19(13), 3454-3457. https://doi.org/10.1021/acs.orglett.7b01393

The cyclic dodecapeptides wewakazole and wewakazole B have been synthesized by a divergent strategy via a common tris-proline containing oxazole octapeptide and two separate bisoxazole containing tetrapeptide units, followed by peptide coupling and m... Read More about Total synthesis of the cyclic dodecapeptides wewakazole and wewakazole B.

Total Synthesis of the Post‐translationally Modified Polyazole Peptide Antibiotic Goadsporin (2017)
Journal Article
Dexter, H. L., Williams, H. E., Lewis, W., & Moody, C. J. (2017). Total Synthesis of the Post‐translationally Modified Polyazole Peptide Antibiotic Goadsporin. Angewandte Chemie International Edition, 56(11), 3069-3073. https://doi.org/10.1002/anie.201612103

The structurally unique polyazole antibiotic goadsporin contains six heteroaromatic oxazole and thiazole rings integrated into a linear array of amino acids that also contains two dehydroalanine residues. An efficient total synthesis of goadsporin is... Read More about Total Synthesis of the Post‐translationally Modified Polyazole Peptide Antibiotic Goadsporin.