Search Results - "Brookfield, Joanna"

Selective Hydroxylation of C(sp3)−H Bonds in Steroids by Abas, Hossay, Blencowe, Peter, Brookfield, Joanna L., Harwood, Lucy A.

“…Steroids are highly prevalent structures in small‐molecule therapeutics, with the level of oxidation being key to their biological activity and physicochemical…”
Get full text

Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3 by Boyd, Scott, Brookfield, Joanna L, Critchlow, Susan E, Cumming, Iain A, Curtis, Nicola J, Debreczeni, Judit, Degorce, Sébastien L, Donald, Craig, Evans, Nicola J, Groombridge, Sam, Hopcroft, Philip, Jones, Neil P, Kettle, Jason G, Lamont, Scott, Lewis, Hilary J, MacFaull, Philip, McLoughlin, Sheila B, Rigoreau, Laurent J. M, Smith, James M, St-Gallay, Steve, Stock, Julie K, Turnbull, Andrew P, Wheatley, Edward R, Winter, Jon, Wingfield, Jonathan

“…A weak screening hit with suboptimal physicochemical properties was optimized against PFKFB3 kinase using critical structure-guided insights. The resulting…”
Get full text

Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties by Charles, Mark D, Brookfield, Joanna L, Ekwuru, Tennyson C, Stockley, Martin, Dunn, John, Riddick, Michelle, Hammonds, Tim, Trivier, Elisabeth, Greenland, Gavin, Wong, Ai Ching, Cheasty, Anne, Boyd, Susan, Crighton, Diane, Olson, Michael F

“…As part of a program to develop a small molecule inhibitor of LIMK, a series of aminothiazole inhibitors were discovered by high throughput screening. Scaffold…”
Get full text

Correction to “Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models” by Finlay, M. Raymond V., Anderton, Mark, Bailey, Andrew, Boyd, Scott, Brookfield, Joanna, Cairnduff, Ceri, Charles, Mark, Cheasty, Anne, Critchlow, Susan E., Culshaw, Janet, Debreczeni, Judit, Ekwuru, Tennyson, Hollingsworth, Ian, Jones, Neil, Leroux, Fred, Littleson, Mairi, McCarron, Hollie, McKelvie, Jennifer, Mooney, Lorraine, Nissink, J. Willem M., Patel, Joe, Perkins, David, Powell, Steve, Quesada, Mar Jimenez, Raubo, Piotr, Sabin, Verity, Smith, James, Smith, Peter D., Stark, Andrew, Ting, Attilla, Wang, Peng, Wilson, Zena, Winter-Holt, Jon J., Wood, J. Matthew, Wrigley, Gail L., Yu, Guoqing, Zhang, Peng

Get full text

Discovery of a Thiadiazole–Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models by Finlay, M. Raymond V, Anderton, Mark, Bailey, Andrew, Boyd, Scott, Brookfield, Joanna, Cairnduff, Ceri, Charles, Mark, Cheasty, Anne, Critchlow, Susan E, Culshaw, Janet, Ekwuru, Tennyson, Hollingsworth, Ian, Jones, Neil, Leroux, Fred, Littleson, Mairi, McCarron, Hollie, McKelvie, Jennifer, Mooney, Lorraine, Nissink, J. Willem M, Perkins, David, Powell, Steve, Quesada, Mar Jimenez, Raubo, Piotr, Sabin, Verity, Smith, James, Smith, Peter D, Stark, Andrew, Ting, Attilla, Wang, Peng, Wilson, Zena, Winter-Holt, Jon J, Wood, J. Matthew, Wrigley, Gail L, Yu, Guoqing, Zhang, Peng

“…Tumors have evolved a variety of methods to reprogram conventional metabolic pathways to favor their own nutritional needs, including glutaminolysis, the first…”
Get full text

LIM kinase inhibitors disrupt mitotic microtubule organization and impair tumor cell proliferation by Mardilovich, Katerina, Baugh, Mark, Crighton, Diane, Kowalczyk, Dominika, Gabrielsen, Mads, Munro, June, Croft, Daniel R, Lourenco, Filipe, James, Daniel, Kalna, Gabriella, McGarry, Lynn, Rath, Oliver, Shanks, Emma, Garnett, Mathew J, McDermott, Ultan, Brookfield, Joanna, Charles, Mark, Hammonds, Tim, Olson, Michael F

“…The actin and microtubule cytoskeletons are critically important for cancer cell proliferation, and drugs that target microtubules are widely-used cancer…”
Get full text

Abstract LB-C20: Lead generation and optimisation of a series of novel glutaminase (GLS) inhibitors by Charles, Mark D., Cairnduff, Ceri, Brookfield, Joanna, Sabin, Verity, Ekwuru, Tennyson, Jones, Neil, Ting, Attilla, Smith, James, Nissink, Willem, Finlay, Ray, Powell, Steve, Critchlow, Susan, Ward, Richard, Wood, Matthew, Ruston, Linette, Winter, Jon, Hollingsworth, Ian

“…Abstract Glutamine is an essential nutrient for cancer cells and is used to support cancer cell growth. Glutamine is converted to glutamate by the enzyme…”
Get full text

Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2- a]pyridine acid pump antagonists (APAs) by Bailey, Nick, Bamford, Mark J., Brissy, Delphine, Brookfield, Joanna, Demont, Emmanuel, Elliott, Richard, Garton, Neil, Farre-Gutierrez, Irene, Hayhow, Thomas, Hutley, Gail, Naylor, Antoinette, Panchal, Terry A., Seow, Hui-Xian, Spalding, David, Takle, Andrew K.

“…A series of novel imidazo[1,2- a]pyridine acid pump antagonists is described. Heteroaryl and heterocyclic substituents at the C-6 position were used for the…”
Get full text

Abstract C210: LIM kinase small molecule inhibitors block tumor cell invasion by Crighton, Diane, Charles, Mark, Trivier, Elizabeth, Hooper, Steven, Scott, Rebecca, Riddick, Michelle, Brookfield, Joanna, Ekwuru, Tennyson, Stockley, Martin, Foxton, Caroline, Williams, Juliet, Raynham, Tony, Sahai, Erik, Olson, Michael, Hammonds, Tim

“…Abstract The invasive potential of carcinomas greatly contributes to their ability to metastasize, a process which is estimated to cause 90% of all human…”
Get full text