School of Life Sciences

Spencer Lab

Welcome to the Spencer group website.
Professor of Bioorganic Chemistry.

see: orcid.org/0000-0001-5231-8836

http://scholar.google.co.uk/citations?user=xYdOQzsAAAAJ&hl=en

 

 

Our work on p53 from a few years ago

 

https://www.youtube.com/watch?v=N4x8LCBoTZI

 

 

Latest news

 

Covid outputs:

https://www.biorxiv.org/content/10.1101/2020.10.29.339317v1?fbclid=IwAR3hMEeX--hM4FEiKNuOMUlq-Lh19o90KrkyNQZN9IaY4VD0Jajb4TsRwd4

>130 scientists involved in a global crowd-sourced consortium to find a covid antiviral. very humbled to be part of this.

 

https://spectrum.ieee.org/the-human-os/artificial-intelligence/medical-ai/covid-moonshot-can-ai-algorithms-and-volunteer-chemists-design-a-knockout-antiviral?fbclid=IwAR04U5yXFfIP3Po0IS-7gEMi4ZZWrfW28_6DOwcytcF_yuQjV3xigJdpmt0

 

CRUK 400K coI (PI Michelle West). Therapeutic Discovery Award from Cancer Research; EBV-targetting small molecules.  2021-2024                                                                 £400K

iCASE Award (2019-) PhD. Started Sept 2019 (GSK/EPSRC) with G Giamas (co-PI).

Thai Royal Government PhD, started.

Leverhulme grant awarded (Spencer, Hughes, Sussex co-Is), Bath lead project. 

Professor Andrew Burrows (PI) University of Bath; The controlled release of semiochemicals from porous materials for pest control; £291,808.

 3 PhDs with Prof Dave Goulson (PI)  (DEFRA and SongBird Survival) awarded.

 lf2  

 We are grateful to the European Regional Development Fund (ERDF) for funding LabFact under the lnterreg V Programme. To find out more about LabFact please go to: www.labfact.eu or e-mail labfact@labfact.eu

 

New papers!


In vivo Active Organometallic-containing Antimycotic Agents. Riccardo Rubbiani, Tobias Weil, Noemi Tocci, Luciano Mastrobuoni, Severin Jeger, Marco Moretto, James Ng, Yan Lin, Jeannine Hess, Stefano Ferrari, Andres Kaech, Luke Young, John Spencer, Anthony Moore, Kevin Cariou, Giorgia Renga, Marilena Pariano, Luigina Romani and Gilles Gasser. RSC Chem. Biol. 2021, accepted, in press. DOI: 10.1039./d1cb00123j.

Rice (Oryza sativa) TIR1 and 5′adamantyl-IAA significantly improve the auxin-inducible degron system in Schizosaccharomyces pombe. Antony M. Watson, Adam T, Hassell-Hart, Storm, Spencer, John and Carr, Tony, Genes, 2021, 12, 6, a882, 1-23.

Synthesis of trans-Mono(silyl)palladium(II) Bromide Complexes Oscar Navarro, John Spencer, Melvyn B. Ansell, George E. Kostakis, Molecules, 2021, 2460.

Genotoxicity and Epigenotoxicity of Carbazole-derived Molecules on MCF-7 Breast Cancer Cells. F. Luparello, C., Cruciata , I., Joerger , A. C., Ocasio, C. A., Jones , R., Khan Tareque, R., Bagley, M. C., Spencer , J., Walker , M., Carol Austin , Ferrara, T., D’Oca, P.,Bellina , R., Branni, R. and Fabio Caradonna. Int. J. Mol. Sci. 2021, 22, 3410.

Probing BRD Inhibition Substituent Effects in Bulky Analogues of (+)‐JQ1. Hassell, Storm; Picaud, Sarah; Lengacher, Ralph; Csuker, Joshua; Millet, Regis; Gasser, Gilles; Alberto, Roger; Maple, Hannah; Felix, Robert; Leśnikowski, Zbigniew; Stewart, Helen; Chevassut, Timothy; Morley, Simon; Filippakopoulos, Panagis*; Spencer, John.* Helv. Chim. Acta. 2021, 104, e2000214.

 

Synthesis and biological evaluation of benzodiazepines containing a pentafluorosulfanyl group, Arathy Jose, Raysa Khan Tareque, Martin Mortensen, Remi Legay, Simon J Coles, Graham J Tizzard, Barnaby W Greenland, Trevor G Smart, Mark C Bagley*, John Spencer*. Tetrahedron, 2021, 132020.

Acetyl-leucine slows disease progression in lysosomal storage disorders. Ecem Kaya, David A. Smith, Claire Smith, Lauren Morris, Tatiana Bremova-Ertl, Mario Cortina-Borja, Paul Fineran, Karl J Morten, Joanna Poulton, Barry Boland, John Spencer, Michael Strupp, Frances M Platt, Brain Commun., 2021, fcaa148, https://doi.org/10.1093/braincomms/fcaa148

The structure-function relationship of oncogenic LMTK3. Angeliki Ditsiou, Chiara Cilibrasi, Nikiana Simigdala, Athanasios Papakyriakou, Leanne Milton Harris, Viviana Vella, Joanne E. Nettleship, Jae Ho Lo, Shivani Soni, Goar Smbatyan, Panagiota Ntavelou, Teresa Gagliano, Maria Chiara Iachini, Sahir Khurshid, Thomas Simon, Lihong Zhou, Storm Hassell-Hart, Philip Carter, Laurence H. Pearl, Robin L. Owen, Raymond J. Owens, S. Mark Roe, Naomi E. Chayen, Heinz-Josef Lenz, John Spencer, Chrisostomos Prodromou, Apostolos Klinakis, Justin Stebbing, Georgios Giamas*. Science Advances, 2020, 6, eabc3099. 

 Raysa Khan Tareque, Storm Hassell-Hart, Tobias Krojer, Anthony Bradley, Srikannathasan Velupillai, Romain Talon, Michael Fairhead,  Iain J. Day, Kamlesh Bala, Robert Felix,  Paul D. Kemmitt,  Paul Brennan,Frank von Delft, Laura Díaz Sáez, Kilian Huber, John Spencer*. Deliberately  Losing  Control  of  C-H  Activation  Processes  in  the Design of Small Molecule Fragment Arrays Targeting Peroxisomal MetabolismChemMedChem, 2020, accepted.  

"turns lemons into lemonade"   

http://practicalfragments.blogspot.com/2021/03/fragment-chemistry-roundup-part-4.html

 

Harina Amer Hamzah,  Daniel Rixson, Joseph Paul-Taylor, Huan V. Doan,  Christopher Dadswell, Gavin W. Roffe,  Arun Sridhar, Claire L. Hobday,  Charlie Wedd,  Tina Düren,  William O. H. Hughes, John Spencer and Andrew D. Burrows * Inclusion and Release Of Ant Alarm Pheromones From Metal–Organic Frameworks.Dalton Trans, 2020, 49 (30), 10334-10338. DOI: 10.1039/d0dt02047h.

 

 

 

  jd1 cryst

jd1Cover Feb 10  2020

Storm Hassell-Hart, Andrew Runcie,Tobias Krojer,  Jordan Doyle, Ella Lineham,  Cory A. Ocasio,  Brenno A. D. Neto, Oleg Fedorov, Graham Marsh, Hannah Maple, Robert Felix, Rebecca Banks, Alessio Ciulli, Sarah Picaud, Panagis Filippakopoulos, Frank von Delft, Paul Brennan,  Helen J. S. Stewart, Timothy J. Chevassut, Martin Walker, Carol Austin, Simon Morley,  and John Spencer*. Synthesis and Biological Investigation of (+)-JD1, an Organometallic BET Bromodomain Inhibitor. Organometallics, 2020, 39, 408-416.

Targeting cavity-creating p53 cancer mutations: the Y220X paradigm. Matthias R. Bauer, Andreas Krämer, Giovanni Settani, Rhiannon N. Jones,  Raysa Khan Tareque, Alan R. Fersht, John Spencer& Andreas C. Joerger, ACS Chem. Biol. 2020, 2020, 15, 3, 657–668. .

Sansook, SupojjaneeHassell-Hart, StormOcasio, Cory and Spencer, John. Ferrocenes in medicinal chemistry; a personal perspective. Journal of Organometallic Chemistry 2020905, 121017.

Bauer, MatthiasJones, Alice RhiannonKhan, RaysaSpringett, BradleyDingler, FelixVerduci, LorenaPatel, KetanFersht, AlanJoerger, Andreas and Spencer, John (2019) A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C. Future Medicinal Chemistry. ISSN 1756-8919 ; (2019) 11(19), 2491–2504

ttps://www.future-science.com/doi/full/10.4155/fmc-2019-0181

OPEN ACCESS!

fmc p53

Commandeur, DanielBrown, GrantMcnulty, PeterDadswell, ChristopherSpencer, John and Chen, Qiao (2019) Yttrium doped ZnO nanorod arrays for increased charge mobility and carrier density for enhanced solar water splitting. The Journal of Physical Chemistry C. ISSN 1932-7455

Spencer, JohnGascon, Jose MiguelOliveri, ValentinaMcGown, AndrewKaya, EcemChen, yu-linAustin, CarolWalker, MartinPlatt, Frances and Vecchio, Graziella (2019) Synthesis and study of novel multifunctional cyclodextrin‐deferasirox hybrids. ChemMedChem. ISSN 1860-7179

OPEN ACCESS!

https://onlinelibrary.wiley.com/doi/full/10.1002/cmdc.201900334

Cover article!

horses

 

 

 

 

 

 

 

Stampani, Stavroula IMcGown, AndrewVargas, AlfredoAbdul-Sada, AlaaTizzard, Graham JColes, Simon JSpencer, John and Kostakis, George E  Solvent-free synthesis and key intermediate isolation in Ni2Dy2 catalyst development in the domino ring-opening electrocyclization reaction of furfural and amines. J. Org. Chem., 2019, 84, 116858-116867.

Neto, Brenno DCarvalho, Pedro H P RCorrea, Jose RPaiva, KarenBaril, MicheleMachado, DanielScholten, Jackson Dde Souza, Paulo Eduardo NarcizoVeiga-Souza, Fabiane and Spencer, John (2019) When the strategies for cellular selectivity fail. Challenges and surprises in the design and application of fluorescent benzothiadiazole derivatives for mitochondrial staining. Org. Chem. Front., 2019, 6, 2371-2384.

Baguña Torres, JuliaYu, ZilinBordoloi, JayantaSunassee, KavithaSmith, DavidSmith, ClaireChen, OscarPurchase, RupertTuschl, KarinSpencer, JohnPlatt, Frances and Blower, Philip J (2019) Imaging of changes in copper trafficking and redistribution in a mouse model of Niemann-Pick C disease using positron emission tomography. BioMetals. https://doi.org/10.1007/s10534-019-00185-5.

Commandeur, DanielBrown, GrantHills, EdwardSpencer, John and Chen, Qiao (2019) Defect-rich ZnO nanorod arrays for efficient solar water splitting. ACS Applied Nano Materials, 2 (3). pp. 1570-1578. 

Luparello, ClaudioAsaro, Dalia Maria LuciaCruciata, IleniaHassell-Hart, StormSansook, SupojjaneeSpencer, Johnand Caradonna, Fabio (2019) Cytotoxic activity of the histone deacetylase 3-Selective inhibitor Pojamide on MDA-MB-231 triple-negative breast cancer cells. International Journal of Molecular Sciences, 20 (4). 804 1-14. 

 

.

 

  

Nice to see one of ours excelling in Niemann Pick C research:

https://www.advancedsciencenews.com/therapeutic-potential-of-cyclodextrins-for-childhood-alzheimers/

 

We're in the news!

http://www.rsc.org/news-events/community/2018/sep/john-spencer-research-fund/

 to

VIP visitor, David De Semir (PHIP collaborator) from California Pacific:

http://cpmcri-currents.org/our-people/discovery-investigators/david-de-semir-phd

 

visit

 

Research Fellow, Raysa:

http://www.sussex.ac.uk/news/all?id=44101

 

New grant:

http://www.sussex.ac.uk/staff/newsandevents/?id=43539?ref=email

 

http://www.theargus.co.uk/NEWS/15892979.Professor___s_hopes_for_new_cancer_treatment_research/

Our new RISE network is now starting on lysosomal storage disorders:

https://lysomod.wixsite.com/lysomod

 

 

 

EPSRC grant awarded!

http://www.sussex.ac.uk/newsandevents/pressrelease/id/40899

http://gow.epsrc.ac.uk/NGBOViewGrant.aspx?GrantRef=EP/P026990/1

https://www.worldwidecancerresearch.org/news/skincancerboost/

 

 EU grant with Southampton, Caen, Rouen:

https://interreg5a-fce.eu/en/projects/approved-projects/view/11/

 

 Invited talk at SCI meeting:

http://www.soci.org/news/young-chemists/epigenetics-2017-preview

2018 Papers

 1. Roffe, Gavin, Boonseng, Sarote, Cox, Hazel and Spencer, John   (2018) Unsymmetrical Pincer palladacycles: synthesis and reactivity.          In:    Morales-Morales, David (ed.)      Pincer compounds: chemistry and applications.            Elsevier.     ISBN 9780128129319     (Accepted)

2. Tuo, Wei, Bollier, Mélanie, Leleu-Chavain, Natascha, Lemaire, Lucas, Barczyk, Amélie, Dezitter, Xavier, Klupsch, Frédérique, Szczepanski, Fabien, Spencer, John, Chavatte, Philippe and Millet, Régis   (2018) Development of novel oxazolo[5,4- d ]pyrimidines as competitive CB 2 neutral antagonists based on scaffold hopping.    European Journal of Medicinal Chemistry.         ISSN 0223-5234    

3. Spencer, John and Walden, Ben, eds.   (2018) Special focus: metals in medicine.    Future Medicinal Chemistry.  10(6), 607–609.    ISSN 1756-8919.

 4. Lineham, Ella, Tizzard, Graham J, Coles, Simon J, Spencer, John and Morley, Simon   (2018) Synergistic effects of inhibiting the MNK-eIF4E and PI3K/AKT/mTOR pathways on cell migration in MDA-MB-231 cells.    Oncotarget.

5. Synthesis and Biological Evaluation of Ferrocene-based Cannabinoid Receptor-2 Ligands Sansook, S.; Wei Tuo, W.; Bollier, M.; Barczyk, A.; Dezitter, X.; Klupsch, F.; Leleu-Chavain, N.; Farce, A.; Tizzard, G. J.; Coles, S. J.; Spencer, J.; Millet, R.*. Fut. Med. Chem. 2018, 10 (6), 631-638.

6. Ansell, M. B., Furfari, S. K.,Cloke, F. G. N.,Roe, S. M., Spencer, J.,* Navarro, O.* Comparison of the Reactivity of the Low Buried-Volume Carbene Complexes (ITMe)2Pd(PhC≡CPh) and (ITMe)2Pd(PhN=NPh). Organometallics. 2018, in press.

 Organomet 2018

 https://twitter.com/Orgmet_ACS/status/980851789175185408 

7.  Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors.  Supojjanee Sansook, Ella Lineham, Storm Hassell-Hart, Graham J. Tizzard, Simon J. Coles, John Spencer* and Simon J. Morley*. Molecules 2018, 23, 2126; doi:10.3390/molecules23092126.

8.  Type II kinase inhibitors targeting Cys-gatekeeper kinases display orthogonality with wild type and Ala/Gly-gatekeeper kinases. Cory A. Ocasio*, Alexander A. Warkentin, Patrick J. McIntyre, Krister J. Barkovich, Clare Vesely, John Spencer, Kevan M. Shokat and Richard Bayliss. ACS Chem. Biol. 2018, 13, 2956−2965.

 asd

 

 2017

1. Transition Metal Catalyzed Hetero Element-Element’ Additions to Alkynes. Ansell, M. B.*; Navarro, O.*; Spencer, J.* Coord. Chem. Rev. 2017, 36, 54-77.

http://dx.doi.org/10.1016/j.ccr.2017.01.003

 

2. A Ruthenium Anticancer Compound Interacts with Histones and Impacts Differently on Epigenetic and Death Pathways Compared to Cisplatin. Licona, C., Spaety M.-E.,, Capuozzo, A., Ali, M.,; Rita, S..; Armat, O..; Delalande, F; Van Dorsselaer, A., Sarah C., Spencer,  J., Pfeffer M., Mellitzer G., Gaiddon C. Oncotarget, 2017, 8 (2), 2568-2584.

http://www.impactjournals.com/oncotarget/index.php?journal=oncotarget&page=article&op=view&path%5b%5d=13711

  onc

 

 3. Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors. Tuo, W.; Leleu-Chavain, N.; Spencer, J.; Sansook, S.; Millet, R.;  Chavatte, P. J. Med. Chem. 2017, 60, 4−46.

4. Rationalization of the Mechanism of in situ Pd(0) Formation for Cross-Coupling Reactions from Novel Unsymmetrical Pincer Palladacycles Using DFT Calculations. Boonseng, S.; Roffe, G. W.; Targema; M.;  Cox, H.; Spencer, J. J. Organomet. Chem. 2017, 845, 71-81.

5.  Khan, R.;  Boonseng, S.;  Kemmitt, P.; Felix, R.; Coles, S. J.; Tizzard, G. J.; Williams, G;  Simmonds, O., Harvey, J.-L.; Atack, J.; Cox, H.; Spencer, J.; Combining Sanford Arylations on Benzodiazepines with the Nuisance Effect. Adv. Synth. Catal. 2017,  359, 3261-3269.

 nuis

http://onlinelibrary.wiley.com/doi/10.1002/adsc.201700626/pdf

 6. Khan, R.; Marsh, G.; Felix, R.; Kemmitt, P. D.; Baud, M. G. J.; Ciulli, A.;  Spencer, J.* Gram Scale Laboratory Synthesis of TC AC 28, a High Affinity BET Bromodomain Ligand. ACS Omega, 20172 (8), pp 4328–4332.

 om

http://pubs.acs.org/doi/abs/10.1021/acsomega.7b00780

 

7. Lineham, Ella, Spencer, John and Morley, Simon   (2017) Dual abrogation of Mnk and mTOR; a novel therapeutic approach for the treatment of aggressive cancers.    Future Medicinal Chemistry.        (Accepted).

8. Pojamide: An HDAC3-Selective Ferrocene Analogue with Remarkably Enhanced Redox-Triggered Ferrocenium Activity in Cells. Cory A. Ocasio, Supojjanee Sansook, Rhiannon Jones, Justin M. Roberts, Thomas G. Scott, Nikolaos Tsoureas, Peter Coxhead, Matthew Guille, Graham J. Tizzard, Simon J. Coles, Helfrid Hochegger, James E. Bradner and John Spencer. Organometallics 2017, 36, 3276–3283.

po

 

9.  N1-Arylation of 1,4-Benzodiazepines with Diaryliodonium Salts. Khan, R.; Felix, R.; Kemmitt, P. D.; Coles, Simon J.; Tizzard, G. J.; Spencer, J.*  Synlett. 2017, accepted, now published, 2018, 29, 193.

synlett 

 

10. Synthesis of Kinase Inhibitors Containing a Pentafluorosulfanyl Moiety. Sansook, S.;  Ocasio, C. A.; Tizzard, G. J.; Coles, S. J.; Fedorov, O.; Bennett, J. M; Elkins, J.; Spencer, J.* Org. Biomol. Chem. 2017, 15, 8655- 8660 .

 sf

 

 

2016 papers

17. Synthesis of Functionalized Hydrazines: Facile Homogenous (N-Heterocyclic Carbene)-Pd(0) Catalyzed Diboration and Silaboration of Azobenzenes. Ansell, M. B.;  Kostakis, G. E.;  Braunschweig, H.*; Navarro,O.*; Spencer, J. * Adv. Synth. Catal. 2016, 358, 3765 –3769.

 

 http://onlinelibrary.wiley.com/doi/10.1002/adsc.201601106/pdf

A most accessed paper of 11/2016: http://onlinelibrary.wiley.com/journal/10.1002/(ISSN)1615-4169/homepage/2258_mostaccessed.html

 

16. Ocasio, Tony, Rajasekaran, Mohan, Walker, Sarah, Le Grand, Darren, Spencer, John, Pearl, Frances, Ward, Simon, Savic, Velibor, Pearl, Laurence, Hochegger, Helfrid and Oliver, Antony (2016) A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct. Oncotarget 2016, 7, 71182-71197.

 

 gwl paper [PDF 6.98MB]

15. Boonseng, Sarote, Roffe, Gavin W, Jones, Rhiannon N, Tizzard, Graham J, Coles, Simon J, Spencer, John and Cox, Hazel (2016) The trans influence in unsymmetrical pincer palladacycles: an experimental and computational study. Inorganics, 4 (25). pp. 1-14. ISSN 2304-6740

 inorgs [PDF 726.38KB]

14. Librizzi, Mariangela, Spencer, John and Luparello, Claudio (2016) Biological effect of a hybrid anticancer agent based on kinase and histone deacetylase inhibitors on triple-negative (MDA-MB231) breast cancer cells. International Journal of Molecular Sciences, 17 (8). p. 1235. ISSN 1422-0067

 

 hybrid [PDF 1.48MB]

13. Close, Adam J, Kemmitt, Paul, Roe, S Mark and Spencer, John (2016) Regioselective routes to orthogonally-substituted aromatic MIDA boronates. Organic and Biomolecular Chemistry, 14 (28). pp. 6751-6756. ISSN 1477-0520

 

12. Close, Adam J, Jones, Rhiannon N, Ocasio, Cory A, Kemmitt, Paul, Roe, S Mark and Spencer, John (2016) Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors. Organic and Biomolecular Chemistry, 14. pp. 8246-8252. ISSN 1477-0520

 

obc [PDF 2.06MB]

 

11. Bauer, Matthias R, Jones, Rhiannon N, Baud, Matthias G J, Wilcken, Rainer, Boeckler, Frank M, Fersht, Alan, Joerger, Andreas C and Spencer, John (2016) Harnessing fluorine-sulfur contacts and multipolar interactions for the design of p53 mutant Y220C rescue drugs. ACS Chemical Biology, 11 (8). pp. 2265-2274. ISSN 1554-8929

 acs chem biol [PDF 2.71MB]

 

 

10. Roffe, Gavin, Tizzard, Graham J, Coles, Simon J, Cox, Hazel and Spencer, John (2016) Synthesis of unsymmetrical NCN′ and PCN pincer palladacycles and their catalytic evaluation compared with a related SCN pincer palladacycle. Organic Chemistry Frontiers, 3. pp. 957-965. ISSN 2052-4110

 

9. Tuschl, Karin, Meyer, Esther, Valdivia, Leonardo E, Zhao, Ningning, Dadswell, Chris, Abdul-Sada, Alaa, Hung, Christina Y, Simpson, Michael A, Chong, W K, Jacques, Thomas S, Woltjer, Randy L, Eaton, Simon, Gregory, Allison, Sanford, Lynn, Kara, Eleanna, Houlden, Henry, Cuno, Stephan M, Prokisch, Holger, Valletta, Lorella, Tiranti, Valeria, Younis, Rasha, Maher, Eamonn R, Spencer, John, Straatman-Iwanowska, Ania, Gissen, Paul, Selim, Laila A M, Pintos-Morell, Guillem, Coroleu-Lletget, Wifredo, Mohammad, Shekeeb S, Yoganathan, Sangeetha, Dale, Russell C, Thomas, Maya, Rihel, Jason, Bodamer, Olaf A, Enns, Caroline A, Hayflick, Susan J, Clayton, Peter T, Mills, Philippa B, Kurian, Manju A and Wilson, Stephen W (2016) Mutations in SLC39A14 disrupt manganese homeostasis and cause childhood-onset parkinsonism–dystonia. Nature Communications, 7. p. 11601. ISSN 2041-1723

 natc [PDF 3.79MB]

8. Spencer, John (2016) [Review] Stefan Bräse (2015) Privileged scaffolds in medicinal chemistry: design, synthesis, evaluation. ChemMedChem, 11 (10). p. 1107. ISSN 1860-7179

 

7. Roffe, Gavin W, Boonseng, Sarote, Baltus, Christine B, Coles, Simon J, Day, Iain, Jones, Rhiannon N, Press, Neil J, Ruiz, Mario, Tizzard, Graham J, Cox, Hazel and Spencer, John (2016) A synthetic, catalytic and theoretical investigation of an unsymmetrical SCN pincer palladacycle. Royal Society Open Science, 3 (4). p. 150656. ISSN 2054-5703

 

open sci [PDF 1.65MB]

6. Ansell, Melvyn B, Spencer, John and Navarro Fernandez, Oscar (2016) (N-heterocyclic carbene)2-Pd(0) catalyzed silaboration of internal and terminal alkynes: scope and mechanistic studies. ACS Catalysis, 6 (4). pp. 2192-2196. ISSN 2155-5435

  

acs cat [PDF 1.47MB]

 

5. Griffiths, Kieran, Dokorou, Vassiliki N, Spencer, John, Abdul-Sada, Alaa, Vargas, Alfredo and Kostakis, George E (2016) Isoskeletal Schiff base polynuclear coordination clusters: synthetic and theoretical aspects. CrystEngComm, 18 (5). pp. 704-713. ISSN 1466-8033

 

4. Khan, Raysa, Felix, Robert, Kemmitt, Paul D, Coles, Simon J, Day, Iain J, Tizzard, Graham J and Spencer, John (2016) Late stage C―H activation of a privileged scaffold; synthesis of a library of benzodiazepines. Advanced Synthesis and Catalysis, 358 (1). pp. 98-109. ISSN 1615-4150

 

raysa asc [PDF 10.98MB]

 

3. Sansook, Supojjanee, Tuo, Wei, Lemaire, Lucas, Tourteau, Aurélien, Barczyk, Amélie, Dezitter, Xavier, Klupsch, Frédérique, Leleu-Chavain, Natascha, Tizzard, Graham J, Coles, Simon J., Millet, Régis and Spencer, John (2016) Synthesis of bioorganometallic nanomolar-potent CB2 agonists containing a ferrocene unit. Organometallics, 35 (19). pp. 3361-3368. ISSN 0276-7333   
  
   
 
  
  
  
    
  
  
  
2. Ansell, Melvyn B, Menezes da Silva, Vitor H, Heerdt, Gabriel, Braga, Ataualpa A C, Spencer, John and Navarro, Oscar (2016) An experimental and theoretical study into the facile, homogenous (N-Heterocyclic Carbene)2-Pd(0) catalyzed diboration of internal and terminal alkynes. Catalysis Science and Technology, 6. pp. 7461-7467. ISSN 2044-4753

 

 cat sci tech [PDF 1.71MB]

1. Cox, Oakley B, Krojer, Tobias, Collins, Patrick, Monteiro, Octovia, Talon, Romain, Bradley, Anthony, Fedorov, Oleg, Amin, Jahangir, Marsden, Brian D, Spencer, John, von Delft, Frank and Brennan, Paul E (2016) A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain. Chemical Science, 7 (3). pp. 2322-2330. ISSN 2041-6520

 phip [PDF 2.58MB]

 

 

See also:

 

http://www.worldwidecancerresearch.org/cancer-research-news/2016/recycle-recycle-recycle

 

 

 

  

 

Congratulations to Poj, who  presented a poster at the 14th Ferrocene colloquium, Konstanz.

http://cms.uni-konstanz.de/14th-ferrocene-colloquium-konstanz-2016/programm/

We are grateful for a Doctoral Overseas Conference (Sussex) for funding this.

 

Melvyn Ansell will spend 3 months in the Braunschweig group, Wurzburg, courtesy of a Royal Society of Chemistry Researcher Mobility grant award

http://www-anorganik.ak-braunschweig.chemie.uni-wuerzburg.de/

 

Gavin Roffe presented a poster entitled ‘A Synthesis, Catalytic Application, and Theoretical Investigation into N’CN, SCN and PCS Pincer Palladacycles’ at:

http://eucomcxxi.webnode.cz/

Again, thanks to Sussex for a travel award!

 

 

 

 

 

 Our 1st paper with LMB from our Worldwide Cancer Research grant now out. Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53. Joerger, A.* C.; Bauer, M. R.; Wilcken, R.; Baud, M. G.; Harbrecht, H.; Exner, T. E.; Boeckler, F. M.; Spencer, J.; Fersht, A. R. Structure, 2015, 23, 2246–2255. (IF=5.6).

http://www.worldwidecancerresearch.org/cancer-research-news/2015/molecular-plaster

 

 

 

 

Group "us"ie; 1-10-14: LHS JS,

 

  

 Meeting with our collaborator Prof Jay Bradner of JQ1 fame. Oxford 2015.

http://www.bradnerlab.org/#about

 

 

 

 

 

A 8-Hydroxyquinoline-Cyclodextrin Conjugate as an Efficient Chelating Agent for
Cobalt(II) and Nickel(II) in Neutral Aqueous Solution. Sgarlata, C.; Oliveri*, V.; Spencer, J. Eur. J. Inorg. Chem. 2015, 5886–5891.

 

 

 

Synthesis of an (NHC)2Pd(SiMe3)2 (NHC = N-Heterocyclic Carbene) Complex. Catalytic, cis-Bis-Silylations of Internal Alkynes with Unactivated Disilanes" Ansell, M. B.; Roberts, D. E.; Cloke, F. G. N.; Navarro, O*.; Spencer, J.* Angew. Chem. Int. Ed. 2015, 54, 5578.

 acie [PDF 3.97MB]

 

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funding has been secured for a 1 year research study. We will investigate metal dyshomeostasis in this disease. project starts Feb 2015.

 

                      

http://www.worldwidecancerresearch.org/research/projects/spencer-molecular-p53 

Yr 2 of the project will commence shortly on p53 mutant rescue with small molecules.

 New PhD:

 A Precompetitive Modular Peptidomimetic Toolkit for Targeting PPIs. iCASE. Welcome and good luck Raysa Khan! Started Sept 2014.

az21

 

 

Papers:

Bismuth coordination Networks Containing Deferiprone: Synthesis, Characterisation, Stability and Antibacterial Activity. Burrows, A. D.; Jurcic, M.; Mahon,M. F.; Pierrat, S.;  Roffe,G. W.; Windle, H.;  Spencer, J. Dalton Trans. 2015, 44, 13814.

The nature of the bonding in symmetrical pincer palladacycles. Boonseng, Sarote, Roffe, Gavin W, Spencer, John and Cox, Hazel. Dalton Trans., 2015, 44. pp. 7570-7577.

Longo, Alessandra, Librizzi, Mariangela, Chuckowree, Irina S, Baltus, Christine B, Spencer, John and Luparello, Claudio (2015) Cytotoxicity of the urokinase-plasminogen activator inhibitor carbamimidothioic acid (4-boronophenyl) methyl ester hydrobromide (BC-11) on triple-negative MDA-MB231 breast cancer cells. Molecules, 20 (6). pp. 9879-9889.

Lemaire, Lucas, Leleu-Chavain, Natascha, Tourteau, Aurélien, Abdul-Sada, Alaa, Spencer, John and Millet, Régis (2015) A rapid route for the preparation of pyrimido[5,4-d]- and pyrido[3,2-d]oxazole. Tetrahedron Letters, 56 (19). pp. 2448-2450

Carbon dots (C-dots) from Cow Manure with Impressive Subcellular Selectivity Tuned by Simple Chemical Modification. Barbosa, C.D. E. S.; Corrêa, J. R.; Medeiros, G. A.; Barreto, G.; Magalhães, K.;  de Oliveira, A. L.;  Spencer, J.;  Rodrigues, M. O.; Neto, B. A. D. Chem. Eur. J. 2015, 21, 5055-5060.

 Seizure Control by Derivatives of Medium Chain Fatty Acids Associated with the Ketogenic Diet Show Novel Branching-Point Structure for Enhanced Potency.  Chang, P.;  Zuckermann, A.; Williams, S.; Close, A. J.; Cano-Jaimez, M.; McEvoy, J. P.;  Spencer, J.; Walker, M. C.; Williams, R. S. B. JPET,  2015, 352 (1), 43-52.

Thermal Analysis of Novel Biphenylamide Derivatives. Owusu-Ware, S. K.; Cherry, A. J.; Baltus, C. B.; Spencer, J.; Antonijevic, M. J. Therm. Anal. Calorim., 2015, 21, 437-452.

Microwave-Mediated Synthesis of N-Methyliminodiacetic Acid (MIDA) Boronates. Close,A. J.; Kemmitt,P.; Emmerson, M. K.; Spencer, J. Tetrahedron, 2014, 70, 9125-9131. 

 

 

 

Synthesis of Hybrid Anticancer Agents Based on Kinase and Histone Deacetylase Inhibitors. Patel, H.; Chuckowree, I.; Coxhead, P. Guille, M.; Wang, M.; Zuckermann, A.;  Williams, R. S. B.;  Librizzi, M.; Paranal, R. N.;  Bradner, J. E.; Spencer, J. MedChemComm. 2014, 5, 1829-1833.

 

Multifunctional 8-Hydroxyquinoline-Appended Cyclodextrins as New Inhibitors of Metal-Induced Protein Aggregation. Oliveri, V.; Attanasio, F.; Puglisi, A.; Spencer, J.; Vecchio, G. Chem. Eur. J., 2014, 20, 8954-8964.

BACK COVER OF JOURNAL and highlighted on the ChemistryViews website:

http://www.chemistryviews.org/details/ezine/6193781/Inhibiting_Protein_Aggregation.html

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The following organisations are thanked for kindly funding our research: 

Oxford Nanopore Technologies RSC- Advancing the Chemical Sciences Tocris - Bioscience  Novartis  BP  Selcia Discoveryaz21              

 

 

 

Contact

Professor John Spencer

Arundel Building
University of Sussex

T +44 1273 877374
E J.Spencer@sussex.ac.uk

Go to John Spencer's profile