1,4-benzodiazepin-2-ones, 1,3,5-benzotriazepines,� atom-economical C–H activation chemistry

Spencer, John, Rathnam, Rajendra P. and Chowdhry, Babur Z. (2010) Methodology issues and design approach of VLE on mathematical concepts acquisition within secondary education in England. Future Medicinal Chemistry, 2 (9). pp. 1441-1449. ISSN 1756-8919 (doi:10.4155/fmc.10.226)

C-C bond formation , C−H bond activation, chelation assistance, palladacycles

Spencer, John (2008) C-H activations via palladacycles. In: Dupont, Jairton and Pfeffer, Michel, (eds.) Palladacycles. Wiley-VCH, Weinheim, pp. 109-121. ISBN 9783527317813 (Print) 9783527623211 (Online) (doi:10.1002/9783527623211.ch6)

CCK, CCK2, gastrin, antagonist, benzotriazepine

Spencer, John, Gaffen, John, Grifin, Eric, Harper, Elaine A., Linney, Ian D., McDonald, Iain M., Roberts, Sonia P., Shaxted, Mark E., Adatia, Trushar and Bashall, Alan (2008) Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template. Bioorganic & Medicinal Chemistry, 16 (6). pp. 2974-2983. ISSN 0968-0896 (doi:10.1016/j.bmc.2007.12.047)

G-protein coupled receptor antagonists, enzyme inhibitors, anticancer agents, palladacycle complexes, synthesis

Spencer, John, Rathnam, Rajendra P. and Chowdhry, Babur Z. (2010) 1,4-Benzodiazipine-2-ones in medicinal chemistry. Future Medicinal Chemistry, 2 (9). pp. 1441-1449. ISSN 1756-8919 (doi:10.4155/fmc.10.226)

HIV treatment, Maraviroc, drug development, CCR5 receptor, HERG

Spencer, John (2009) Case study on Maraviroc, a CCR5 Antagonist for HIV treatment. In: Patrick, Graham L., (ed.) An introduction to medicinal chemistry. Oxford University Press, Oxford, Web update. ISBN 9780199234479

Indolin-2-one (oxindole), Knoevenagel condensation, ferrocene-1,1′-dicarbaldehyde

Spencer, John, Nielsen, Birthe ORCID: https://orcid.org/0000-0002-0849-4987, Thomas, Michael J.K., Male, Louise and Coles, Simon J. (2011) The Knoevenagel product of indolin-2-one and ferrocene-1,1′-dicarbaldehyde. Acta Crystallographica Section C, 67 (7). m245-m248. ISSN 0108-2701 (doi:10.1107/S0108270111021536)

MESG, PNP enzyme, ESI, tuberculosis

Neto, Brenno A.D., Lapis, Alexandre A.M., Netz, Paulo A., Spencer, John, Dias, Silvio L.P., Tamborim, Silvia M., Basso, Luiz A., Santos, Diógenes S. and Dupont, Jairton (2010) Synthesis and enzymatic evaluation of the guanosine analogue 2-amino-6-mercapto-7-methylpurine ribonucleoside (MESG): insights into the phosphorolysis reaction mechanism based on the blueprint transition state: SN1 or SN2? Journal of the Brazilian Chemical Society, 21 (1). pp. 151-156. ISSN 0103-5053 (Print), 1678-4790 (Online) (doi:10.1590/S0103-50532010000100022)

Suzuki coupling, microwave, boronic acid, nucleophilic substitution, biaryls, supported reagents

Spencer, John, Baltus, Christine B., Patel, Hiren, Press, Neil J., Callear, Samantha K., Male, Louise and Coles, Simon J. (2010) Microwave-mediated synthesis of an arylboronate library. ACS Combinatorial Science, 2011 (13):1. pp. 24-31. ISSN 2156-8952 (Print), 2156-8944 (Online) (doi:10.1021/co100011g)

Suzuki–Miyaura coupling, biaryl, piperazine, microwave

Spencer, John, Baltus, Christine B., Press, Neil J., Harrington, Ross W. and Clegg, William (2011) Synthesis of a (piperazin-1-ylmethyl)biaryl library via microwave-mediated Suzuki-Miyaura cross-couplings. Tetrahedron Letters, 52 (31). pp. 3963-3968. ISSN 0040-4039 (online) (doi:10.1016/j.tetlet.2011.05.025)

allylic rearrangement; aldol reaction; CC bond formation; oxidation reaction; palladacycles; pincer complexes

Spencer, John (2008) Other uses of palladacycles in synthesis. In: Dupont, Jairton and Pfeffer, Michel, (eds.) Palladacycles. Wiley-VCH, Weinheim, pp. 227-238. ISBN 9783527317813 (Print) 9783527623211 (Online) (doi:10.1002/9783527623211.ch10)

amines, microwave,molybdenum, nitroarenes, reductions

Spencer, John, Anjum, Nazira, Patel, Hiren, Rathnam, Rajendra and Verma, Jason (2007) Molybdenum hexacarbonyl and DBU reduction of nitro compounds under microwave irradiation. Synlett, 2007 (16). pp. 2557-2558. ISSN 0936-5214 (doi:10.1055/s-2007-986628)

amines, reduction, molybdenum, microwave, nitroaromatics

Spencer, John, Rathnam, Rajendra, Patel, Hiren and Anjum, Nazira (2008) Microwave mediated reduction of heterocycle and fluorine containing nitroaromatics with Mo(CO)(6) and DBU. Tetrahedron, 64 (44). pp. 10195-10200. ISSN 0040-4020 (doi:10.1016/j.tet.2008.08.036)

benzodiazepine, C-H activation, palladium, catalysis

Spencer, John, Chowdhry, Babur Z., Mallet, Anthony I., Rathnam, Rajendra P., Adatia, Trushar, Bashall, Alan and Rominger, Frank (2008) C-H activations on a 1H-1,4-benzodiazepin-2(3H)-one template. Tetrahedron, 64 (26). pp. 6082-6089. ISSN 0040-4020 (doi:10.1016/j.tet.2008.01.059)

benzodiazepine, cutaneous leishmaniasis

Parbhu Patel, Asha, Deacon, Andrew D., Spencer, John, Raj, Rathnam, Harbige, Laurence and Getti, Giulia ORCID: https://orcid.org/0000-0003-1402-8496 (2010) The benzodiazepine class of compounds as a potential for the treatment of cutaneous leishmaniasis. In: XII International Congress of Parasitology ICOPA, 15 - 20 Aug 2010, Melbourne, Australia. (Unpublished)

bioinorganic chemistry, ruthenium, metallacycles, antitumor agents

Leyva, Lida, Sirlin, Claude, Rubio, Laura, Franco, Cecilia, Le Lagadec, Ronan, Spencer, John, Bischoff, Pierre, Gaiddon, Christian, Loeffler, Jean-Philippe and Pfeffer, Michel (2007) Synthesis of cycloruthenated compounds as potential anticancer agents. European Journal of Inorganic Chemistry, 2007 (19). pp. 3055-3066. ISSN 1434-1948 (doi:10.1002/ejic.200601149)

biphenyls, stability, polymorphs, thermal analysis

Owusu-Ware, Samuel K., Masud, Mohammed, Baltus, Christine, Spencer, John and Antonijevic, Milan ORCID: https://orcid.org/0000-0002-5847-7886 (2011) Thermal stability implication of positional isomerism of novel biphenyl derivatives. In: 2011 AAPS Annual Meeting and Exposition, 23-27 Oct 2011, Washington Convention Center, Washington, D.C., USA. (Unpublished)

biphenyls, thermal analysis, polymorphs

Cherry, A., Amin, B., Baltus, C., Spencer, J. and Antonijevic, M. ORCID: https://orcid.org/0000-0002-5847-7886 (2011) Thermal analysis of a polymorphic biphenyl structural motifs. In: Published Meeting Abstracts [AAPS]. The AAPS Journal, 2011 . American Association of Pharmaceutical Scientists (AAPS), Arlington, VA, USA. ISSN 1550-7416

chemistry, organic

Puglisi, Antonino, Spencer, John, Oliveri, Valentina, Vecchio, Graziella, Kong, Xiaole, Clarke, James and Milton, John (2011) Synthesis, physicochemical properties and antioxidant activity of deferiprone-cyclodextrin conjugates and their iron(iii) complexes. Dalton Transactions, 41 (10). pp. 2877-2883. ISSN 1477-9226 (Print), 1477-9234 (Online) (doi:10.1039/c1dt11677k)

cross coupling, microwaves, biphenylamides, hydrogen bonds, Z', X-ray crystallography

Baltus, Christine, Press, Neil J., Antonijevic, Milan D. ORCID: https://orcid.org/0000-0002-5847-7886, Tizzard, Graham J., Coles, Simon J. and Spencer, John (2012) Synthesis of a biphenyl library for studies of hydrogen bonding in the solid state. Tetrahedron, 68 (45). pp. 9272-9277. ISSN 0040-4020 (doi:10.1016/j.tet.2012.08.062)

crystal structure, palladacycle, 2-(Thiophen-2-yl)pyridine, dimer, Triphenylphosphine

Callear, Samantha K., Spencer, John, Patel, Hiren, Deadman, John J. and Hursthouse, Michael B. (2010) Crystal structures of two palladacycles from the C-H activation of 2-(Thiophen-2-yl)pyridine. Journal of Chemical Crystallography, 41 (4). pp. 523-527. ISSN 1074-1542 (Print), 1572-8854 (Online) (doi:10.1007/s10870-010-9913-5)

cyclic di-amino acid peptide, cyclic dipeptides, x-ray crystal structure, absolute configuration, DKP ring conformations

Mendham, Andrew P., Spencer, John, Chowdhry, Babur Z., Dines, Trevor J., Mujahid, Muhammad, Palmer, Rex A., Tizzard, Graham J. and Coles, Simon J. (2011) X-ray crystallographic structure and absolute configuration of the cyclic Di-amino acid peptide: Cyclo(L-HomoCySH-L-HomoCySH). Journal of Chemical Crystallography, 41 (9). pp. 1328-1334. ISSN 1074-1542 (Print), 1572-8854 (Online) (doi:10.1007/s10870-011-0098-3)

cyclic dipeptide, cyclic di-amino acid peptide, x-ray crystal structure, DKP ring conformations

Mendham, Andrew P., Spencer, John, Chowdhry, Babur Z., Dines, Trevor J., Mujahid, Muhammad, Palmer, Rex A., Tizzard, Graham J. and Coles, Simon J. (2011) X-ray crystallographic structure of the cyclic di-amino acid peptide: N,N′-Diacetyl-cyclo(Gly-Gly). Journal of Chemical Crystallography, 41 (9). pp. 1323-1327. ISSN 1074-1542 (Print), 1572-8854 (Online) (doi:10.1007/s10870-011-0097-4)

estrogen-receptor modulators, tyrosine kinase-activity, breast-cancer, in-vitro, inhibitors, antimalarial, chloroquine, ferrocifens, activation, chemistry

Spencer, John, Mendham, Andrew P., Kotha, Arun K., Richardson, Simon C.W. ORCID: https://orcid.org/0000-0002-7927-0649, Hillard, Elizabeth A., Jaouen, Gérard, Male, Louise and Hursthouse, Michael B. (2008) Structural and biological investigation of ferrocene-substituted 3-methylidene-1,3-dihydro-2H-indol-2-ones. Dalton Transactions, 2009 (6). pp. 918-921. ISSN 1477-9226 (Print), 1477-9234 (Online) (doi:10.1039/B816249B)

ferrocene, HDAC inhibitor, bioinorganic, anticancer, hydroxamic acid

Spencer, John, Amin, Jahangir, Wang, Minghua, Packham, Graham, Syed Alwi, Sharifah S., Tizzard, Graham J., Coles, Simon J., Paranal, Ronald M., Bradner, James E. and Heightman, Tom D. (2011) Synthesis and biological evaluation of JAHAs: ferrocene-based histone deacetylase inhibitors. ACS Medicinal Chemistry Letters, 2 (5). pp. 358-362. ISSN 1948-5875 (doi:10.1021.ml100295v)

ferrocene-based 1,2,3-triazole-containing hydroxamic acids, click chemistry, HDAC inhibition and activity

Spencer, John, Amin, Jahangir, Boddiboyena, Ramesh, Packham, Graham, Cavell, Breeze E., Alwi, Sharifah S. Syed, Paranal, Ronald M., Heightman, Tom D., Wang, Minghua, Marsden, Brian, Coxhead, Peter, Guille, Matthew, Tizzard, Graham J., Coles, Simon J. and Bradner, James E, (2012) Click JAHAs: Conformationally restricted ferrocene-based histone deacetylase inhibitors. Medicinal Chemistry Communication, 3 (1). pp. 61-64. ISSN 2040-2503 (online) (doi:10.1039/c1md00203a)

growth-factor receptor, microwave irradiation, pi interactions, reduction, bond, dbu

Spencer, John, Chowdhry, Babur Z., Hamid, Samiyah, Mendham, Andrew P., Male, Louise, Coles, Simon J. and Hursthouse, Michael B. (2010) Seven 3-methylidene-1H-indol-2(3H)-ones related to the multiple-receptor tyrosine kinase inhibitor sunitinib. Acta Crystallographica Section C: Crystal Structure Communications, 66 (2). o71-o78. ISSN 0108-2701 (Print), 1600-5759 (Online) (doi:10.1107/S0108270109054134)

heterocycles, microwaves, parallel synthesis, piperazines, flow chemistry

Spencer, John, Patel, Hiren, Callear, Samantha K., Coles, Simon J. and Deadman, John J. (2011) Synthesis and solid state study of pyridine- and pyrimidine-based fragment libraries. Tetrahedron Letters, 52 (45). pp. 5905-5909. ISSN 0040-4039 (online) (doi:10.1016/j.tetlet.2011.07.147)

lysosomal cysteine proteases, bioorganometallic chemistry, breast-cancer, complexes, progression, drugs, pharmaceuticals

Spencer, John, Casini, Angela, Zava, Olivier, Rathnam, Rajendra P., Velhanda, Santosh K., Pfeffer, Michel, Callear, Samantha K., Hursthouse, Michael B. and Dyson, Paul J. (2009) Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles. Dalton Transactions (48). pp. 10731-10735. ISSN 1477-9226 (Print), 1477-9234 (Online) (doi:10.1039/b912096c)

metallocene, kinase inhibitor, 3-Methylidene-Oxindoles

Spencer, John, Amin, Jahangir, Coxhead, Peter, McGeehan, John, Richards, Christopher J., Tizzard, Graham J., Coles, Simon J., Bingham, John P., Hartley, John A., Feng, Li, Meggers, Eric and Guille, Matthew (2011) Size does matter. Sterically demanding metallocene-substituted 3-methylidene-oxindoles exhibit poor kinase inhibitory action. Organometallics, 30 (11). pp. 3177-3181. ISSN 0276-7333 (Print), 1520-6041 (Online) (doi:10.1021/om200278j)

metals, oncology, cancer, metallodrugs

Spencer, John (2009) Current metallodrugs in cancer. In: Patrick, Graham L., (ed.) An introduction to medicinal chemistry. Oxford University Press, Oxford, Web update. ISBN 9780199234479

microwave, medicinal chemistry

Spencer, John (2009) Microwave technology applied to medicinal chemistry. In: Patrick, Graham L., (ed.) An introduction to medicinal chemistry. Oxford University Press, Oxford, Web update. ISBN 9780199234479

microwave-assisted synthesis, 6-amino-β-cyclodextrins, functionalised cyclodextrins, mono-pendant cyclodextrins

Puglisi, Antonino, Spencer, John, Clark, James and Milton, John (2011) Microwave-assisted synthesis of 6-amino-β-cyclodextrins. Journal of Inclusion Phenomena and Macrocyclic Chemistry, 73 (1-4). pp. 475-478. ISSN 0923-0750 (Print), 1573-1111 (Online) (doi:10.1007/s10847-011-0054-z)

microwave-assisted synthesis, oxazoles, parallel synthesis, flow chemistry

Spencer, John, Patel, Hiren, Amin, Jahangir, Callear, Samantha K., Coles, Simon J. and Deadman, John J. (2012) Microwave-mediated synthesis and manipulation of a 2-substituted-5-aminooxazole-4-carbonitrile library. Tetrahedron Letters, 53 (13). pp. 1656-1659. ISSN 0040-4039 (doi:10.1016/j.tetlet.2012.01.081)

microwave-mediated chemistry, stoichiometric reducing agent, anilines, chemoselectivity, steric hindrance, halide substituents (I, Br, Cl or F), SNAr/reduction processes, palladium-catalyzed coupling, submicromolar antitrypanosomal activity

Spencer, John (2010) Research spotlight: Microwave chemistry enabling the synthesis of biologically relevant amines. Future Medicinal Chemistry, 2 (2). pp. 161-168. ISSN 1756-8919 (Print), 1756-8927 (Online) (doi:10.4155/fmc.09.114)

microwaves, parallel synthesis, heterocycles, amides, cyclisation

Chuckowree, Irina, Ali Syed, Murtaza, Getti, Giulia ORCID: https://orcid.org/0000-0003-1402-8496, Parbhu Patel, Asha, Garner, Hannah, Tizzard, Graham J., Coles, Simon J. and Spencer, John (2012) Synthesis of a 1,3,5-benzotriazepine-2,4-dione based library. Tetrahedron Letters, 53 (28). pp. 3607-3611. ISSN 0040-4039 (doi:10.1016/j.tetlet.2012.05.025)

monoclonal-antibody, protein, growth, ramps, cells, pthrp, bone, osteoprotegerin, specificity, metastasis

McDonald, Iain M., Austin, Carol, Buck, Ildiko M., Dunstone, David J., Gaffen, John, Griffin, Eric, Harper, Elaine A., Hull, Robert A.D., Kalindjian, S. Barret, Linney, Ian D., Low, Caroline M.R., Patel, Dipa, Pether, Michael J., Raynor, Michelle, Roberts, Sonia P., Shaxted, Mark E., Spencer, John, Steel, Katherine I.M., Sykes, David A., Wright, Paul T. and Xun, Wei (2007) [Letter] Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists. Journal of Medicinal Chemistry, 50 (20). pp. 4789-4792. ISSN 0022-2623 (Print), 1520-4804 (Online) (doi:10.1021/jm0707626)

nitroarenes, anilines, microwave-mediated chemistry, molybdenum hexacarbonyl

Spencer, John (2010) Microwave chemistry enabling the synthesis of biologically relevant amines. Future Medicinal Chemistry, 2 (2). pp. 161-168. ISSN 1756-8919 (Print), 1756-8927 (Online) (doi:10.4155/fmc.09.114)

organometallic chemistry, antitumor-activity, complexes, drugs, precatalysts, inhibitors, palladium, design, agents

Spencer, John, Rathnam, Rajendra P., Montukuri, Mahesh, Kotha, Arun K., Richardson, Simon C.W. ORCID: https://orcid.org/0000-0002-7927-0649, Hazrati, Ali, Hartley, John A., Male, Louise and Hursthouse, Michael B. (2009) Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity. Dalton Transactions (22). pp. 4299-4303. ISSN 1477-9226 (Print), 1477-9234 (Online) (doi:10.1039/b819061e)

parallel synthesis, microwaves, benzodiazepines, trypanosoma

Spencer, John, Rathnam, Rajendra P., Harvey, Alan L., Clements, Carol J., Clark, Rachel L., Barrett, Michael P., Wong, Pui Ee, Male, Louise, Coles, Simon J. and Mackay, Simon P. (2011) Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity. Bioorganic & Medicinal Chemistry, 19 (5). pp. 1802-1815. ISSN 0968-0896 (doi:10.1016/j.bmc.2011.01.010)

pincer, organometallic complexes,

Dupont, Jairton, Consorti, C. and Spencer, John (2007) Organometallic pincer-type complexes: recent applications in synthesis and catalysis. In: Morales-Morales, David and Jensen, Craig M., (eds.) The Chemistry of Pincer Compounds. Elsevier, Amsterdam, pp. 1-24. ISBN 9780444531384 (doi:10.1016/B978-044453138-4/50002-7)

receptor antagonists, conference report

Spencer, John (2010) Conference report: 7th Annual Congress of International Drug Discovery Science and Technology. Future Medicinal Chemistry, 2 (1). pp. 21-23. ISSN 1756-8919 (doi:10.4155/FMC.09.151)

synthesis

Spencer, John (2009) Combinatorial and parallel synthesis. In: Patrick, Graham L., (ed.) An introduction to medicinal chemistry. Oxford University Press, Oxford, pp. 307-331. ISBN 9780199234479

synthesis, evaluation, metallocene, methylidene-1,3-dihydro-2H-indol-2-ones, kinase inhibitors

Spencer, John, Amin, Jahangir, Callear, Samantha K., Tizzard, Graham J., Coles, Simon J., Coxhead, Peter and Guille, Matthew (2011) Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors. Metallomics, 3 (6). pp. 600-608. ISSN 1756-5901 (doi:10.1039/C1MT00017A)