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

 

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

 

New EPSRC grant just 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.

 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,