All Outputs (6)

Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones (2022)
Journal Article
Mehmood, H., Musa, M., Woodward, S., Hossan, M. S., Bradshaw, T. D., Haroon, M., …Akhtar, T. (2022). Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones. RSC Advances, 12(52), 34126-34141. https://doi.org/10.1039/d2ra03226k

Cyclization of substituted thiosemicarbazones with α-bromo-4-cyanoacetophenone allows rapid single-step sustainable syntheses of 4-cyanophenyl-2-hydrazinylthiazoles libraries (30 examples, 66–79%). All show anticancer efficacy against HCT-116 and MCF... Read More about Design, and synthesis of selectively anticancer 4-cyanophenyl substituted thiazol-2-ylhydrazones.

Synthesis of Quinolone Antibiotic Analogues: A Multistep Synthetic Chemistry Experiment for Undergraduates (2021)
Journal Article
Bailie, A. E., & Nortcliffe, A. (2021). Synthesis of Quinolone Antibiotic Analogues: A Multistep Synthetic Chemistry Experiment for Undergraduates. Journal of Chemical Education, 98(10), 3333-3340. https://doi.org/10.1021/acs.jchemed.1c00459

A multistep synthesis of quinolone antibiotic analogues was developed as a laboratory experiment for intermediate/advanced undergraduate students. Students can synthesize a range of desfluoroenoxacin analogues via a five-step sequence. The experiment... Read More about Synthesis of Quinolone Antibiotic Analogues: A Multistep Synthetic Chemistry Experiment for Undergraduates.

Iridum-catalysed C–H Borylation of β-aryl-aminopropionic acids (2020)
Journal Article
Robinson, H., Stillibrand, J., Simelis, K., Macdonald, S. J., & Nortcliffe, A. (2020). Iridum-catalysed C–H Borylation of β-aryl-aminopropionic acids. Organic and Biomolecular Chemistry, 18, https://doi.org/10.1039/d0ob01495h

Iridium-catalysed catalytic, regioselective C–H borylation of β-aryl-aminopropionic acid derivatives gives access to 3,5-functionalised protected β-aryl-aminopropionic acid boronates. The synthetic versatility of these new boronates is demonstrated t... Read More about Iridum-catalysed C–H Borylation of β-aryl-aminopropionic acids.

Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery (2018)
Journal Article
Santos, M. S., Nortcliffe, A., Lewis, W., Bradshaw, T. D., & Moody, C. J. (in press). Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery. Chemistry - A European Journal, https://doi.org/10.1002/chem.201801309

1,2-Diazetidin-3-ones are readily accessible, small ring scaffolds that upon functionalization have the potential to produce diverse 3-dimensional structures for drug discovery. Thus treatment of diazo hydrazides, obtained from simple hydrazides and... Read More about Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery.

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.

Seven-membered ring scaffolds for drug discovery: Access to functionalised azepanes and oxepanes through diazocarbonyl chemistry (2015)
Journal Article
Nortcliffe, A., & Moody, C. J. (2015). Seven-membered ring scaffolds for drug discovery: Access to functionalised azepanes and oxepanes through diazocarbonyl chemistry. Bioorganic and Medicinal Chemistry, 23(11), 2730-2735. https://doi.org/10.1016/j.bmc.2015.01.010

© 2015 Elsevier Ltd. All rights reserved. Functionalised azepane and oxepane scaffolds were prepared using diazocarbonyl chemistry and elaborated to show their potential use in library synthesis. Key dicarbonyl containing seven-membered rings were fu... Read More about Seven-membered ring scaffolds for drug discovery: Access to functionalised azepanes and oxepanes through diazocarbonyl chemistry.