Search Results - "Fillery, Shaun M"

A Buchwald–Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3‐Ligase PROTACs by Hayhow, Thomas G., Borrows, Rachel E. A., Diène, Coura R., Fairley, Gary, Fallan, Charlene, Fillery, Shaun M., Scott, James S., Watson, David W.

“…A palladium‐catalysed Buchwald–Hartwig amination for lenalidomide‐derived aryl bromides was optimised using high throughput experimentation (HTE). The…”
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Expeditious Access to Functionalized Tricyclic Pyrrolo-Pyridones via Tandem or Sequential C–N/C–C Bond Formations by Fillery, Shaun M, Gregson, Clare L, Guérot, Carine M

“…The facile synthesis of both saturated and unsaturated tricyclic pyrrolo-pyridones starting from a single readily available, common monocyclic reagent has been…”
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Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase by Bagal, Sharan K, Gregson, Clare, O’ Donovan, Daniel H, Pike, Kurt G, Bloecher, Andrew, Barton, Peter, Borodovsky, Alexandra, Code, Erin, Fillery, Shaun M, Hsu, Jessie Hao-Ru, Kawatkar, Sameer P, Li, Chengzhi, Longmire, David, Nai, Youfeng, Nash, Samuel C, Pike, Andrew, Robinson, James, Read, Jon A, Rawlins, Phillip B, Shen, Minhui, Tang, Jia, Wang, Peng, Woods, Haley, Williamson, Beth

“…Aberrant activity of the histone methyltransferase polycomb repressive complex 2 (PRC2) has been linked to several cancers, with small-molecule inhibitors of…”
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Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models by Winter-Holt, Jon J, Bardelle, Catherine, Chiarparin, Elisabetta, Dale, Ian L, Davey, Paul R. J, Davies, Nichola L, Denz, Christopher, Fillery, Shaun M, Guérot, Carine M, Han, Fujin, Hughes, Samantha J, Kulkarni, Meghana, Liu, Zhaoqun, Milbradt, Alexander, Moss, Thomas A, Niu, Huijun, Patel, Joe, Rabow, Alfred A, Schimpl, Marianne, Shi, Junjie, Sun, Dongqing, Yang, Dejian, Guichard, Sylvie

“…ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncology target. While…”
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Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor by Finlay, M. Raymond V., Buttar, David, Critchlow, Susan E., Dishington, Allan P., Fillery, Shaun M., Fisher, Eric, Glossop, Steve C., Graham, Mark A., Johnson, Trevor, Lamont, Gillian M., Mutton, Simon, Perkins, Paula, Pike, Kurt G., Slater, Anthony M.

“…The identification of mTOR kinase inhibitor hits from HTS screening and their development into leads such as 32 is described High throughput screening to…”
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Amination of ethers using chloramine-T hydrate and a copper(I) catalyst by Albone, David P, Challenger, Stephen, Derrick, Andrew M, Fillery, Shaun M, Irwin, Jacob L, Parsons, Christopher M, Takada, Hiroya, Taylor, Paul C, Wilson, D James

“…Amination of C-H bonds activated by ether oxygen atoms is facile with chloramine-T as nitrene source and copper(I) chloride in acetonitrile as catalyst. For…”
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Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas by Burrows, Jeremy N., Cumming, John G., Fillery, Shaun M., Hamlin, Gordon A., Hudson, Julian A., Jackson, Ruth J., McLaughlin, Sharon, Shaw, John S.

“…Investigation of weak screening hits led to the identification of N-alkyl- N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides and N-alkyl-…”
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Ring expansion of 5- to 6-member zirconacycles by carbenoid insertion by Dixon, Sally, Fillery, Shaun M., Kasatkin, Aleksandra, Norton, David, Thomas, Emma, Whitby, Richard J.

“…A wide range of carbenoids (1-lithio-1-halo species), including those with α-SiR 3, OEt, SPh, SO 2Ph, P(O)(OEt) 2, and CN substituents, insert into 5-member…”
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Facile synthesis of 3-alkoxyindoles via rhodium(II)-catalysed diazoindole O–H insertion reactions by Kettle, Jason G, Faull, Alan W, Fillery, Shaun M, Flynn, Anthony P, Hoyle, Marcus A, Hudson, Julian A

“…2-Carboethoxy-3-diazo-3 H-indole is a substrate for rhodium(II)-catalysed alcohol O–H insertion reactions leading to 3-alkoxyindoles in good yield. The scope…”
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Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries by Burton, Rebecca J., Crowther, Mandy L., Fazakerley, Neal J., Fillery, Shaun M., Hayter, Barry M., Kettle, Jason G., McMillan, Caroline A., Perkins, Paula, Robins, Peter, Smith, Peter M., Williams, Emma J., Wrigley, Gail L.

“…The highly regioselective Buchwald–Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and…”
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