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Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists (2017)
Journal Article
Kindon, N., Andrews, G., Baxter, A., Cheshire, D., Hemsley, P., Johnson, T., …Stocks, M. J. (in press). Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists. ACS Medicinal Chemistry Letters, 8(9), 981–986. https://doi.org/10.1021/acsmedchemlett.7b00315

N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high throughput screen (HTS) of a sub-set of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excelle... Read More about Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists.

Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers (2017)
Journal Article
Panduga, V., Stocks, M. J., & Bosquillon, C. (2017). Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers. International Journal of Pharmaceutics, 532(1), https://doi.org/10.1016/j.ijpharm.2017.08.112

The mechanism by which quaternized anticholinergic bronchodilators permeate the airway epithelium remains controversial to date. In order to elucidate the role of drug transporters, ipratropium bidirectional transport as well as accumulation and rele... Read More about Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers.

Drug-like antagonists of P2Y receptors — from lead identification to drug development (2016)
Journal Article
Conroy, S., Kindon, N., Kellam, B., & Stocks, M. (in press). Drug-like antagonists of P2Y receptors — from lead identification to drug development. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.5b01972

P2Y receptors are expressed in virtually all cells and tissue types and mediate an astonishing array of biological functions, including platelet aggregation, smooth muscle cell proliferation, and immune regulation. The P2Y receptors belong to the G p... Read More about Drug-like antagonists of P2Y receptors — from lead identification to drug development.

Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery (2015)
Journal Article
Stone, E. L., Citossi, F., Singh, R., Kaur, B., Gaskell, M., Farmer, P. B., …Bradshaw, T. D. (2015). Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery. Bioorganic and Medicinal Chemistry, 23(21), 6891-6899. https://doi.org/10.1016/j.bmc.2015.09.052

Potent, selective antitumour AhR ligands 5F 203 and GW 610 are bioactivated by CYPs 1A1 and 2W1. Herein we reason that DNA adducts’ generation resulting in lethal DNA double strand breaks (DSBs) underlies benzothiazoles’ activity. Treatment of sensit... Read More about Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery.

Linifanib – a multi-targeted receptor tyrosine kinase inhibitor and a low molecular weight gelator (2015)
Journal Article
Marlow, M., Al-Ameedee, M., Smith, T., Wheeler, S., & Stocks, M. J. (in press). Linifanib – a multi-targeted receptor tyrosine kinase inhibitor and a low molecular weight gelator. Chemical Communications, 51, https://doi.org/10.1039/c5cc00454c

In this study we demonstrate that linifanib, a multi-targeted receptor tyrosine kinase inhibitor, with a key urea containing pharmacophore, self-assembles into a hydrogel in the presence of low amounts of solvent. We demonstrate the role of the urea... Read More about Linifanib – a multi-targeted receptor tyrosine kinase inhibitor and a low molecular weight gelator.

Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold (2015)
Journal Article
Schwehm, C., Li, J., Song, H., Hu, X., Kellam, B., & Stocks, M. (2015). Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold. ACS Medicinal Chemistry Letters, 6(3), https://doi.org/10.1021/ml500503n

A novel molecular scaffold has been synthesized and its synthesis and incorporation into new analogues of biologically active molecules will be discussed. A comparison of the inhibitory activity of these compounds to the known type-2 diabetes compoun... Read More about Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold.

Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action (2014)
Journal Article
Stocks, M., Alcaraz, L., Bailey, A., Bonnert, R., Cadogan, E., Christie, J., …Young, A. (2014). Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action. ACS Medicinal Chemistry Letters, 5(4), 416-421. https://doi.org/10.1021/ml4005232

A series of dibasic des-hydroxy β2 receptor agonists has been prepared and evaluated for potential as inhaled ultra-long acting bronchodilators. Determination of activities at the human β-adrenoreceptors demonstrated a series of highly potent and se... Read More about Discovery of AZD3199, An Inhaled Ultralong Acting β2 Receptor Agonist with Rapid Onset of Action.