Dr James Wilkinson's Outputs (15)

Development of a novel and versatile synthesis for a potentially therapeutic di-aryl-alkylamine and related analogues (2024)
Thesis

Fendiline is an obsolete ion channel inhibitor originally prescribed as an anti-hypertensive medicine. However, recent repurposing has shown promising efficacy towards a range of serious ailments, most notably carcinomas including pancreatic and colo... Read More about Development of a novel and versatile synthesis for a potentially therapeutic di-aryl-alkylamine and related analogues.

Synthesis non-sugar GAG mimetics (2023)
Thesis

The Met receptor is a well-known motility, metastasis, and apoptosis modulator within
human cells. Its activity is known to be accelerated in cancer cells. Its activation has been
found to be co-dependent on the attachment of the hepatocyte growth... Read More about Synthesis non-sugar GAG mimetics.

Targeting c-met in sonic hedgehog medulloblastomas (2022)
Thesis
Morlando, S. Targeting c-met in sonic hedgehog medulloblastomas. (Thesis). University of Salford

Medulloblastoma (MB), a cerebellar tumour primarily diagnosed in children, is the most common malignant brain tumour consisting of four molecular subgroups: Wingless (WNT), Sonic Hedgehog (SHH), Group 3 and Group 4. Although the 70-75% of MB patients... Read More about Targeting c-met in sonic hedgehog medulloblastomas.

Novel copper-catalysed coupling reactions of diphenylmethane (2021)
Thesis
Breski, A. (in press). Novel copper-catalysed coupling reactions of diphenylmethane. (Dissertation). University of Salford

In this thesis, a novel synthesis of the drug fendiline was attempted. Fendiline was sold commercially as an angina therapeutic, and recent studies have shown that it is also anti-malarial and has activity against cancers with a high mortality rate.... Read More about Novel copper-catalysed coupling reactions of diphenylmethane.

Establishing a structure-activity-relationship for small molecule non-sugar glycomimetics (2021)
Thesis
Dobiecki-Davies, J. Establishing a structure-activity-relationship for small molecule non-sugar glycomimetics. (Dissertation). University of Salford

DAOY Medullablastoma cells are highly invasive, mobile and can cause severe neurological and physical illness in patients affected by this cancer. Previous work by Wilkinson & Co-workers (2017) showed that some small-molecule non-sugar glycomimetic d... Read More about Establishing a structure-activity-relationship for small molecule non-sugar glycomimetics.

Synthesis of small-molecule HGF-Met inhibitors for use in preventing cell motility (2020)
Thesis
Bunte, A. Synthesis of small-molecule HGF-Met inhibitors for use in preventing cell motility. (Dissertation). University of Salford

Glycosaminoglycans are becoming more and more focused upon as a research topic due to the broad use they have in aiding wound healing and preventing cell motility through competitive inhibition of the HGF-Met pathway. This pathway is extremely import... Read More about Synthesis of small-molecule HGF-Met inhibitors for use in preventing cell motility.

Lead optimisation of dehydroemetine for repositioned use in malaria (2020)
Journal Article

Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel anti-malarial treatments. The anti-amoebic compound, emetine dihydrochloride, has been identified as a potent in-vitro inhibitor of the mult... Read More about Lead optimisation of dehydroemetine for repositioned use in malaria.

Investigating the anti-proliferative properties and their mechanism(s) of action of marine derived glycosaminoglycans from two marine sources (2020)
Thesis
two marine sources. (Dissertation). University of Salford

The purpose of this study was to investigate the chemotherapeutic properties of marine derived glycosaminoglycans (GAGs) and investigate their mechanism(s) of action. The secondary purpose was to investigate differences between the already studied co... Read More about Investigating the anti-proliferative properties and their mechanism(s) of action of marine derived glycosaminoglycans from two marine sources.

A novel role for small molecule glycomimetics in the protection against lipid-induced endothelial dysfunction : Involvement of Akt/eNOS and Nrf2/ARE signaling (2016)
Journal Article

Background: Glycomimetics are a diverse array of saccharide-inspired compounds, designed to mimic the bioactive
functions of glycosaminoglycans. Therefore, glycomimetics represent a unique source of novel therapies to
target aberrant signaling and... Read More about A novel role for small molecule glycomimetics in the protection against lipid-induced endothelial dysfunction : Involvement of Akt/eNOS and Nrf2/ARE signaling.

Expanding the scope of the Babler-Daubin oxidation : 1,3-oxidative transposition of secondary allylic alcohols (2016)
Journal Article
Killoran, P., Rossington, S., Wilkinson, J., & Hadfield, J. (2016). Expanding the scope of the Babler-Daubin oxidation : 1,3-oxidative transposition of secondary allylic alcohols. Tetrahedron Letters, 57(35), 3954-3957. https://doi.org/10.1016/j.tetlet.2016.07.076

We report the catalytic chromium-mediated oxidation of secondary allylic alcohols to give α,β-unsaturated aldehydes with exclusive (E)-stereoselectivity. This facile procedure employs catalytic PCC (5 mol%) and periodic acid (H5IO6) as a co-oxidant.... Read More about Expanding the scope of the Babler-Daubin oxidation : 1,3-oxidative transposition of secondary allylic alcohols.

Asymmetric synthesis of diarylmethane derivatives by dynamic kinetic resolution (2015)
Journal Article
kinetic resolution. Tetrahedron Letters, 56(26), 4025-4027. https://doi.org/10.1016/j.tetlet.2015.05.006

Asymmetric allylation of ortho-methoxydiphenylmethane has been carried out with high yields and ee of up to 94% using the chiral ligand (−)-sparteine as an additive. Results of reactions performed under various conditions suggest that a dynamic kinet... Read More about Asymmetric synthesis of diarylmethane derivatives by dynamic kinetic resolution.

Asymmetric alkylation of diarylmethane derivatives (2006)
Journal Article
Wilkinson, J., Rossington, S., Ducki, S., Leonard, J., & Hussain, N. (2006). Asymmetric alkylation of diarylmethane derivatives. Tetrahedron, 62(8), 1833-1844. https://doi.org/10.1016/j.tet.2005.11.044

Deprotonation–alkylation of prochiral diarylmethane substrates using sec-BuLi and (−)-sparteine has been carried out in excellent yields and up to 94% ee. A variety of enantioselective alkylations, silylations and stannylations have been performed on... Read More about Asymmetric alkylation of diarylmethane derivatives.

Towards the total synthesis of tangutorine by intramolecular Diels–Alder reaction (2005)
Journal Article
Wilkinson, J., Ardes-Guisot, N., Ducki, S., & Leonard, J. (2005). Towards the total synthesis of tangutorine by intramolecular Diels–Alder reaction. Tetrahedron Letters, 46(46), 8053-8056. https://doi.org/10.1016/j.tetlet.2005.09.058

The syntheses of 3,5-disubstituted-2-sulfolenes, and their participation in Pictet-Spengler reactions to give precursors of tangutorine, are described.

Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent (2004)
Journal Article
Wilkinson, J., Rossington, S., Leonard, J., & Hussain, N. (2004). Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent. Tetrahedron Letters, 45(28), 5481-5483. https://doi.org/10.1016/j.tetlet.2004.05.058

Alkylation of 2-methoxyethoxyphenyl phenyl methane using sec-BuLi and (−)-sparteine has been carried out in excellent yields and up to 94% ee. The best results were obtained in allylation reactions but methylation, ethylation, benzylation and trimeth... Read More about Asymmetric alkylation of diarylmethane derivatives. Improved results using methoxyethoxy substituent.

Asymmetric alkylation of diphenylmethane derivatives using (-)-sparteine (2004)
Journal Article
Wilkinson, J., Rossington, S., Leonard, J., & Hussain, N. (2004). Asymmetric alkylation of diphenylmethane derivatives using (-)-sparteine. Tetrahedron Letters, 45(6), 1191-1193. https://doi.org/10.1016/j.tetlet.2003.11.138

Alkylation of 2-oxygenated diphenylmethane derivatives using sec-butyllithium and (−)-sparteine gave enantiomeric excesses of up to 60% with allyl bromide but alkylations with methyl electrophiles were poorly selective. When compounds with a free hyd... Read More about Asymmetric alkylation of diphenylmethane derivatives using (-)-sparteine.