List of works - John Spencer

1,4-Benzodiazepin-2-Ones in Medicinal Chemistry ⬇️

scientific article (publication date: September 2010)

A cyclodextrin-capped histone deacetylase inhibitor.

scientific article published on 2 April 2013

A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct

scientific article

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c5sc03115j.

scientific article published on 22 December 2015

A ruthenium anticancer compound interacts with histones and impacts differently on epigenetic and death pathways compared to cisplatin.

scientific article

A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C

scientific article published on 01 October 2019

A synthetic, catalytic and theoretical investigation of an unsymmetrical SCN pincer palladacycle

scientific article

Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template.

scientific article published on 25 December 2007

Biological Effect of a Hybrid Anticancer Agent Based on Kinase and Histone Deacetylase Inhibitors on Triple-Negative (MDA-MB231) Breast Cancer Cells.

scientific article published on 30 July 2016

Bismuth coordination networks containing deferiprone: synthesis, characterisation, stability and antibacterial activity

scientific article published on 01 August 2015

Boron medicinal chemistry and synthetic aspects

scientific article published in April 2013

Carbon dots (C-dots) from cow manure with impressive subcellular selectivity tuned by simple chemical modification

scientific article published on 18 February 2015

Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors

Cytotoxic Activity of the Histone Deacetylase 3-Selective Inhibitor Pojamide on MDA-MB-231 Triple-Negative Breast Cancer Cells

scientific article published on 13 February 2019

Cytotoxic effects of Jay Amin hydroxamic acid (JAHA), a ferrocene-based class I histone deacetylase inhibitor, on triple-negative MDA-MB231 breast cancer cells

scientific article published in November 2012

Cytotoxicity of the Urokinase-Plasminogen Activator Inhibitor Carbamimidothioic Acid (4-Boronophenyl) Methyl Ester Hydrobromide (BC-11) on Triple-Negative MDA-MB231 Breast Cancer Cells.

scientific article published on 28 May 2015

Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors

scientific article published on 25 July 2016

Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

scientific article

Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53.

scientific article published on December 2015

G-Protein Coupled Receptor and Kinase Targets: Advances in Drug Discovery from Molecular to Clinical ⬇️

scientific article published on July 1, 2011

Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

scientific article published on 08 August 2017

Harnessing Fluorine-Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs

scientific article

Highlights from SelectBio 2015: Academic Drug Discovery Conference, Cambridge, UK, 19-20 May 2015.

scientific article published on 30 September 2015

Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT.

scientific article

Imaging of changes in copper trafficking and redistribution in a mouse model of Niemann-Pick C disease using positron emission tomography

scientific article published on 07 March 2019

Inclusion and release of ant alarm pheromones from metal-organic frameworks

scientific article published on 21 July 2020

Incorporation by coordination and release of the iron chelator drug deferiprone from zinc-based metal-organic frameworks.

scientific article

Isoskeletal Schiff base polynuclear coordination clusters: synthetic and theoretical aspects

scientific article published in 2016

Late Stage CH Activation of a Privileged Scaffold; Synthesis of a Library of Benzodiazepines

Microwave-mediated synthesis and manipulation of a 2-substituted-5-aminooxazole-4-carbonitrile library

Microwave-mediated synthesis of an arylboronate library

scientific article

Molecular Signatures Associated with Treatment of Triple-Negative MDA-MB231 Breast Cancer Cells with Histone Deacetylase Inhibitors JAHA and SAHA.

scientific article published on 12 November 2017

Multifunctional 8-hydroxyquinoline-appended cyclodextrins as new inhibitors of metal-induced protein aggregation

scientific article published on 26 May 2014

Mutations in SLC39A14 disrupt manganese homeostasis and cause childhood-onset parkinsonism-dystonia

scientific article

N1-Arylation of 1,4-Benzodiazepine-2-ones with Diaryliodonium Salts

New cyclodextrin-bearing 8-hydroxyquinoline ligands as multifunctional molecules

scientific article published on 22 August 2013

Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.

scientific article published on April 2006

Olefin cross-metathesis/Suzuki–Miyaura reactions on vinylphenylboronic acid pinacol esters

On the noninnocent nature of 1,3-dialkylimidazolium ionic liquids

scientific article published on 01 October 2004

Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion

scientific article published on 31 May 2007

Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors

scientific article published on 23 August 2018

Prodrug and covalent linker strategies for the solubilization of dual-action antioxidants/iron chelators.

scientific article published in November 2002

Recent advances in the development of selective CB(2) agonists as promising anti-inflammatory agents.

scientific article published on January 2012

Regioselective routes to orthogonally-substituted aromatic MIDA boronates

scientific article published on 01 July 2016

Research spotlight: Microwave chemistry enabling the synthesis of biologically relevant amines.

scientific article

Seizure control by derivatives of medium chain fatty acids associated with the ketogenic diet show novel branching-point structure for enhanced potency.

scientific article published on 17 October 2014

Seven 3-methylidene-1H-indol-2(3H)-ones related to the multiple-receptor tyrosine kinase inhibitor sunitinib

scientific article published on 15 January 2010

Size Does Matter. Sterically Demanding Metallocene-Substituted 3-Methylidene-Oxindoles Exhibit Poor Kinase Inhibitory Action

Small molecule induced reactivation of mutant p53 in cancer cells

scientific article

Solvent-Free Synthesis and Key Intermediate Isolation in Ni2Dy2 Catalyst Development in the Domino Ring-Opening Electrocyclization Reaction of Furfural and Amines

scientific article published on 22 May 2019

Solvent‐Free Synthesis of Core‐Functionalised Naphthalene Diimides by Using a Vibratory Ball Mill: Suzuki, Sonogashira and Buchwald–Hartwig Reactions

scientific article published in 2022

Structural and biological investigation of ferrocene-substituted 3-methylidene-1,3-dihydro-2H-indol-2-ones

scientific article

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

scientific article

Synthesis and Study of Multifunctional Cyclodextrin-Deferasirox Hybrids

scientific article published on 24 June 2019

Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

scientific article

Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors.

scientific article

Synthesis and solid state study of pyridine- and pyrimidine-based fragment libraries

Synthesis and solid-state characterisation of 4-substituted methylidene oxindoles

scientific article published on 20 December 2013

Synthesis of Bioorganometallic Nanomolar-Potent CB2 Agonists Containing a Ferrocene Unit

Synthesis of Functionalized Hydrazines: Facile Homogeneous (N-Heterocyclic Carbene)-Palladium(0)-Catalyzed Diboration and Silaboration of Azobenzenes ⬇️

scientific article published on 9 November 2016

Synthesis of Oxindole-Based Bioorganometallic Kinase Inhibitors Incorporating One or More Ferrocene Groups

Synthesis of P,S,O-ligands incorporating a planar chiral ferrocenyl motif

scientific article published in January 1996

Synthesis of a (piperazin-1-ylmethyl)biaryl library via microwave-mediated Suzuki–Miyaura cross-couplings

Synthesis of a 1,3,5-benzotriazepine-2,4-dione based library

Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity.

scientific article

Synthesis of a biphenyl library for studies of hydrogen bonding in the solid state

Synthesis of an [(NHC)2 Pd(SiMe3 )2 ] Complex and Catalytic cis-Bis(silyl)ations of Alkynes with Unactivated Disilanes.

scientific article published on 9 April 2015

Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

scientific article published on 6 October 2017

Synthesis of unsymmetrical NCN′ and PCN pincer palladacycles and their catalytic evaluation compared with a related SCN pincer palladacycle

Synthesis, physicochemical properties and antioxidant activity of deferiprone-cyclodextrin conjugates and their iron(III) complexes

scientific article published on 30 November 2011

Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm

scientific article published on 21 February 2020

Targeting Epidermal Growth Factor Receptor with Ferrocene-Based Kinase Inhibitors

The Histone Deacetylase Inhibitor JAHA Down-Regulates pERK and Global DNA Methylation in MDA-MB231 Breast Cancer Cells.

scientific article published on 16 October 2015

The Knoevenagel product of indolin-2-one and ferrocene-1,1′-dicarbaldehyde

scientific article published on 25 June 2011

The Trans Influence in Unsymmetrical Pincer Palladacycles: An Experimental and Computational Study

The nature of the bonding in symmetrical pincer palladacycles

scientific article published on 01 April 2015

The potential of palladacycles: more than just precatalysts.

scientific article

The structure-function relationship of oncogenic LMTK3

scientific article published on 13 November 2020

The unexpected but predictable tetrazole packing in flexible 1-benzyl-1H-tetrazole

Type II Kinase Inhibitors Targeting Cys-Gatekeeper Kinases Display Orthogonality with Wild Type and Ala/Gly-Gatekeeper Kinases ⬇️

scientific article published on 09 October 2018

Welcome to ‘Microwaves in Medicinal Chemistry‘ ⬇️

scientific article published on February 1, 2010

List of works by John Spencer

1,4-Benzodiazepin-2-Ones in Medicinal Chemistry ⬇️

A cyclodextrin-capped histone deacetylase inhibitor.

A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c5sc03115j.

A ruthenium anticancer compound interacts with histones and impacts differently on epigenetic and death pathways compared to cisplatin.

A structure-guided molecular chaperone approach for restoring the transcriptional activity of the p53 cancer mutant Y220C

A synthetic, catalytic and theoretical investigation of an unsymmetrical SCN pincer palladacycle

Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template.

Biological Effect of a Hybrid Anticancer Agent Based on Kinase and Histone Deacetylase Inhibitors on Triple-Negative (MDA-MB231) Breast Cancer Cells.

Bismuth coordination networks containing deferiprone: synthesis, characterisation, stability and antibacterial activity

Boron medicinal chemistry and synthetic aspects

Carbon dots (C-dots) from cow manure with impressive subcellular selectivity tuned by simple chemical modification

Click JAHAs: conformationally restricted ferrocene-based histone deacetylase inhibitors

Cytotoxic Activity of the Histone Deacetylase 3-Selective Inhibitor Pojamide on MDA-MB-231 Triple-Negative Breast Cancer Cells

Cytotoxic effects of Jay Amin hydroxamic acid (JAHA), a ferrocene-based class I histone deacetylase inhibitor, on triple-negative MDA-MB231 breast cancer cells

Cytotoxicity of the Urokinase-Plasminogen Activator Inhibitor Carbamimidothioic Acid (4-Boronophenyl) Methyl Ester Hydrobromide (BC-11) on Triple-Negative MDA-MB231 Breast Cancer Cells.

Elaboration of tetra-orthogonally-substituted aromatic scaffolds towards novel EGFR-kinase inhibitors

Excellent correlation between cathepsin B inhibition and cytotoxicity for a series of palladacycles

Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53.

G-Protein Coupled Receptor and Kinase Targets: Advances in Drug Discovery from Molecular to Clinical ⬇️

Gram-Scale Laboratory Synthesis of TC AC 28, a High-Affinity BET Bromodomain Ligand

Harnessing Fluorine-Sulfur Contacts and Multipolar Interactions for the Design of p53 Mutant Y220C Rescue Drugs

Highlights from SelectBio 2015: Academic Drug Discovery Conference, Cambridge, UK, 19-20 May 2015.

Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT.

Imaging of changes in copper trafficking and redistribution in a mouse model of Niemann-Pick C disease using positron emission tomography

Inclusion and release of ant alarm pheromones from metal-organic frameworks

Incorporation by coordination and release of the iron chelator drug deferiprone from zinc-based metal-organic frameworks.

Isoskeletal Schiff base polynuclear coordination clusters: synthetic and theoretical aspects

Late Stage CH Activation of a Privileged Scaffold; Synthesis of a Library of Benzodiazepines

Microwave-mediated synthesis and manipulation of a 2-substituted-5-aminooxazole-4-carbonitrile library

Microwave-mediated synthesis of an arylboronate library

Molecular Signatures Associated with Treatment of Triple-Negative MDA-MB231 Breast Cancer Cells with Histone Deacetylase Inhibitors JAHA and SAHA.

Multifunctional 8-hydroxyquinoline-appended cyclodextrins as new inhibitors of metal-induced protein aggregation

Mutations in SLC39A14 disrupt manganese homeostasis and cause childhood-onset parkinsonism-dystonia

N1-Arylation of 1,4-Benzodiazepine-2-ones with Diaryliodonium Salts

New cyclodextrin-bearing 8-hydroxyquinoline ligands as multifunctional molecules

Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.

Olefin cross-metathesis/Suzuki–Miyaura reactions on vinylphenylboronic acid pinacol esters

On the noninnocent nature of 1,3-dialkylimidazolium ionic liquids

Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion

Probing the Anticancer Action of Novel Ferrocene Analogues of MNK Inhibitors

Prodrug and covalent linker strategies for the solubilization of dual-action antioxidants/iron chelators.

Recent advances in the development of selective CB(2) agonists as promising anti-inflammatory agents.

Regioselective routes to orthogonally-substituted aromatic MIDA boronates

Research spotlight: Microwave chemistry enabling the synthesis of biologically relevant amines.

Seizure control by derivatives of medium chain fatty acids associated with the ketogenic diet show novel branching-point structure for enhanced potency.

Seven 3-methylidene-1H-indol-2(3H)-ones related to the multiple-receptor tyrosine kinase inhibitor sunitinib

Size Does Matter. Sterically Demanding Metallocene-Substituted 3-Methylidene-Oxindoles Exhibit Poor Kinase Inhibitory Action

Small molecule induced reactivation of mutant p53 in cancer cells

Solvent-Free Synthesis and Key Intermediate Isolation in Ni2Dy2 Catalyst Development in the Domino Ring-Opening Electrocyclization Reaction of Furfural and Amines

Solvent‐Free Synthesis of Core‐Functionalised Naphthalene Diimides by Using a Vibratory Ball Mill: Suzuki, Sonogashira and Buchwald–Hartwig Reactions

Structural and biological investigation of ferrocene-substituted 3-methylidene-1,3-dihydro-2H-indol-2-ones

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

Synthesis and Study of Multifunctional Cyclodextrin-Deferasirox Hybrids

Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity

Synthesis and evaluation of metallocene containing methylidene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors.

Synthesis and solid state study of pyridine- and pyrimidine-based fragment libraries

Synthesis and solid-state characterisation of 4-substituted methylidene oxindoles

Synthesis of Bioorganometallic Nanomolar-Potent CB2 Agonists Containing a Ferrocene Unit

Synthesis of Functionalized Hydrazines: Facile Homogeneous (N-Heterocyclic Carbene)-Palladium(0)-Catalyzed Diboration and Silaboration of Azobenzenes ⬇️

Synthesis of Oxindole-Based Bioorganometallic Kinase Inhibitors Incorporating One or More Ferrocene Groups

Synthesis of P,S,O-ligands incorporating a planar chiral ferrocenyl motif

Synthesis of a (piperazin-1-ylmethyl)biaryl library via microwave-mediated Suzuki–Miyaura cross-couplings

Synthesis of a 1,3,5-benzotriazepine-2,4-dione based library

Synthesis of a 1,4-benzodiazepine containing palladacycle with in vitro anticancer and cathepsin B activity.

Synthesis of a biphenyl library for studies of hydrogen bonding in the solid state

Synthesis of an [(NHC)2 Pd(SiMe3 )2 ] Complex and Catalytic cis-Bis(silyl)ations of Alkynes with Unactivated Disilanes.

Synthesis of kinase inhibitors containing a pentafluorosulfanyl moiety

Synthesis of unsymmetrical NCN′ and PCN pincer palladacycles and their catalytic evaluation compared with a related SCN pincer palladacycle

Synthesis, physicochemical properties and antioxidant activity of deferiprone-cyclodextrin conjugates and their iron(III) complexes

Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm

Targeting Epidermal Growth Factor Receptor with Ferrocene-Based Kinase Inhibitors

The Histone Deacetylase Inhibitor JAHA Down-Regulates pERK and Global DNA Methylation in MDA-MB231 Breast Cancer Cells.

The Knoevenagel product of indolin-2-one and ferrocene-1,1′-dicarbaldehyde

The Trans Influence in Unsymmetrical Pincer Palladacycles: An Experimental and Computational Study

The nature of the bonding in symmetrical pincer palladacycles

The potential of palladacycles: more than just precatalysts.

The structure-function relationship of oncogenic LMTK3

The unexpected but predictable tetrazole packing in flexible 1-benzyl-1H-tetrazole