All Outputs (3)

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.