A. Hayes

发表

The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK1 Inhibitor SAR-020106

Gary Box, Ian Collins, Melanie Valenti, 2010, Molecular Cancer Therapeutics.

Molecular Cancer Therapeutics The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK 1 Inhibitor SAR-020106

M. Walton, K. Boxall, G. Aherne, 2009 .

Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone.

X. Barril, B. Davis, M. Drysdale, 2009, Journal of Medicinal Chemistry.

CCT244747 Is a Novel Potent and Selective CHK1 Inhibitor with Oral Efficacy Alone and in Combination with Genotoxic Anticancer Drugs

S. Robinson, M. Walton, K. Boxall, 2012, Clinical Cancer Research.

4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer.

Mike Wood, Brian Dymock, Xavier Barril, 2007, Journal of medicinal chemistry.

NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis.

L. Pearl, X. Barril, M. Drysdale, 2008, Cancer research.

Targeting the Hsp90 molecular chaperone with novel macrolactams. Synthesis, structural, binding, and cellular studies.

L. Pearl, P. Workman, W. Aherne, 2011, ACS chemical biology.

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Gary Box, Paul Workman, Christian Wiesmann, 2008, Journal of medicinal chemistry.

Small Molecule Antagonists of the σ-1 Receptor Cause Selective Release of the Death Program in Tumor and Self-Reliant Cells and Inhibit Tumor Growth in Vitro and in Vivo

A. Prescott, A. Thompson, C. Downes, 2004, Cancer Research.

Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-roscovitine in the mouse.

D. Lane, P. Workman, P. Fischer, 2005, Molecular cancer therapeutics.

A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity

I. Vivanco, F. Raynaud, B. Schwartz, 2020, British Journal of Cancer.

A cell-based screening method using an intracellular antibody for discovering small molecules targeting the translocation protein LMO2

T. Rabbitts, Ami Miller, F. Raynaud, 2021, Science Advances.

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

A. Faisal, M. Valenti, A. K. de Haven Brandon, 2017, British Journal of Cancer.

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach.

R. V. van Montfort, A. Faisal, N. Cronin, 2016, Journal of medicinal chemistry.

Peritumoral Delivery of Docetaxel‐TIPS Microparticles for Prostate Cancer Adjuvant Therapy

H. Ahmed, Alan T. Henley, F. Raynaud, 2020, Advanced therapeutics.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

S. Robinson, R. V. van Montfort, M. Lamers, 2016, Journal of medicinal chemistry.

Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Journal of medicinal chemistry.

Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2021, Journal of medicinal chemistry.

Evaluation of the cassette dosing approach for assessing the pharmacokinetics of geldanamycin analogues in mice

P. Workman, F. Raynaud, A. Hayes, 2004, Cancer Chemotherapy and Pharmacology.

Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1

R. V. van Montfort, F. Raynaud, A. Hayes, 2021, Bioorganic & medicinal chemistry letters.

Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2022, Scientific Reports.

Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases.

M. Waterfield, P. Workman, P. Parker, 2007, Cancer research.

Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941

P. Workman, Irina S. Chuckowree, P. Clarke, 2009, Molecular Cancer Therapeutics.

Discovery of 3-Alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as Selective, Orally Bioavailable CHK1 Inhibitors

M. Walton, K. Boxall, G. Aherne, 2012, Journal of medicinal chemistry.

Pentafluoronitrobenzene a novel scaffold for the solid-phase synthesis of 2,4,6-substituted-3,5-difluoronitrobenzene libraries

I. Hardcastle, A. Hayes, M. Jarman, 2002 .

Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.

P. Workman, P. Clarke, F. Raynaud, 2011, Bioorganic & medicinal chemistry.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen

R. V. van Montfort, P. Workman, R. T. te Poele, 2016, Journal of medicinal chemistry.

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.

Paul Workman, Peter M Fischer, Wayne Jackson, 2011, Bioorganic & medicinal chemistry.

FGF7–FGFR2 autocrine signaling increases growth and chemoresistance of fusion‐positive rhabdomyosarcomas

A. Kelsey, M. Valenti, F. Raynaud, 2021, Molecular oncology.

Achieving In Vivo Target Depletion through the Discovery and Optimization of Benzimidazolone BCL6 Degraders

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2020, Journal of medicinal chemistry.

The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eμ-MYC driven B-cell lymphoma

M. Walton, N. Perkins, K. Boxall, 2015, Oncotarget.

In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.

L. Pearl, P. Workman, R. Marais, 2007, Cancer research.

Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.

L. Pearl, A. Oliver, K. Boxall, 2011, Journal of medicinal chemistry.

Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing

Gary Box, Ian Collins, Isaac M. Westwood, 2011, Journal of medicinal chemistry.

Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution

Y. Le Bihan, Alan T. Henley, F. Raynaud, 2016, Xenobiotica; the fate of foreign compounds in biological systems.

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

R. V. van Montfort, A. Faisal, F. Raynaud, 2019, Molecular Cancer Therapeutics.

Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors

M. Drysdale, P. Workman, Alan T. Henley, 2006, Molecular Cancer Therapeutics.

Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026

P. Workman, L. Kèlland, F. Raynaud, 2005, British Journal of Cancer.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4-d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)

R. V. van Montfort, A. Faisal, N. Cronin, 2018, Journal of medicinal chemistry.

Structure Enabled Design of BAZ2-ICR, A Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B

Lewis R. Vidler, Stefan Knapp, Susanne Müller, 2015, Journal of medicinal chemistry.

Structure-Based Design of Orally Bioavailable 1H-Pyrrolo[3,2-c]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

Isaac M. Westwood, Julian Blagg, Florence I. Raynaud, 2013, Journal of medicinal chemistry.

Synthesis of a benzoxazinthione derivative of tanaproget and pharmacological evaluation for PET imaging of PR expression

F. Raynaud, A. Hayes, C. Cawthorne, 2019, EJNMMI Radiopharmacy and Chemistry.

C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

G. F. Ruda, O. Fedorov, O. Rossanese, 2019, European journal of medicinal chemistry.

Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

O. Rossanese, Benjamin R Bellenie, R. V. van Montfort, 2023, Journal of Medicinal Chemistry.

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues

L. Pearl, X. Barril, M. Drysdale, 2007, Molecular Cancer Therapeutics.

A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity

I. Vivanco, F. Raynaud, B. Schwartz, 2020, British Journal of Cancer.

Discovery and validation of biomarkers to support clinical development of NXP800: A first-in-class orally active, small-molecule HSF1 pathway inhibitor

P. Workman, P. Clarke, M. Valenti, 2022, European Journal of Cancer.

The discovery of GDC-0941: A potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

M. Zvelebil, P. Workman, T. Hancox, 2008 .

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

A. Faisal, M. Valenti, A. K. de Haven Brandon, 2017, British Journal of Cancer.

iTAG an optimized IMiD-induced degron for targeted protein degradation in human and murine cells

T. Westbrook, R. V. van Montfort, Y. Le Bihan, 2023, iScience.

Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases

Paul Workman, Bissan Al-Lazikani, Sibylle Mittnacht, 2019, bioRxiv.

HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies

P. Workman, P. Clarke, Alan T. Henley, 2023, Journal of medicinal chemistry.

ALK2 inhibitors display beneficial effects in preclinical models of ACVR1 mutant diffuse intrinsic pontine glioma

M. Monje, J. Mora, Chris Jones, 2019, Communications Biology.

Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species

A. Faisal, F. Raynaud, A. Hayes, 2019, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

Competitive SPR using an intracellular anti-LMO2 antibody identifies novel LMO2-interacting compounds

T. Rabbitts, Ami Miller, F. Raynaud, 2021, Journal of immunological methods.

Fragment docking supported by NMR shift perturbations

B. Davis, M. Drysdale, M. Jensen, 2014 .

Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941

P. Workman, Irina S. Chuckowree, P. Clarke, 2009, Molecular Cancer Therapeutics.

Small molecule antagonists of the sigma-1 receptor cause selective release of the death program in tumor and self-reliant cells and inhibit tumor growth in vitro and in vivo.

A. Prescott, A. Thompson, C. Downes, 2004, Cancer research.

Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9

Alan T. Henley, A. Hayes, S. Sharp, 2016, MedChemComm.

Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).

R. V. van Montfort, K. Boxall, G. Aherne, 2016, Journal of medicinal chemistry.

Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase

H. Rzepa, A. Hayes, R. Burke, 2024, Journal of medicinal chemistry.

CCT244747 Is a Novel Potent and Selective CHK1 Inhibitor with Oral Efficacy Alone and in Combination with Genotoxic Anticancer Drugs

S. Robinson, M. Walton, K. Boxall, 2012, Clinical Cancer Research.