B. Dymock

发表

Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.

Chang Kai Soh, A. Poulsen, Meredith Williams, 2012, Bioorganic & medicinal chemistry letters.

Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.

Kay Lin Goh, Z. Bonday, J. Wood, 2011, Journal of medicinal chemistry.

SB1578, a Novel Inhibitor of JAK2, FLT3, and c-Fms for the Treatment of Rheumatoid Arthritis

J. Wood, A. William, B. Dymock, 2012, The Journal of Immunology.

Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms.

X. Barril, M. Drysdale, P. Workman, 2004, Chemistry & biology.

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.

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.

Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design.

Xavier Barril, Paul Workman, Roderick E Hubbard, 2005, Journal of medicinal chemistry.

Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.

J. Yen, A. Poulsen, B. Dymock, 2016, Journal of medicinal chemistry.

Emerging therapies for hepatitis C virus infection

B. Dymock, Brian W Dymock, 2001, Expert opinion on emerging drugs.

Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 – 2012

B. Dymock, Cheng Shang See, 2013, Expert opinion on therapeutic patents.

Recent News in the Fast-Paced Field of JAK Inhibitors

B. Dymock, 2013 .

Hydrogen sulfide is an endogenous regulator of aging in Caenorhabditis elegans.

S. Stürzenbaum, B. Halliwell, P. Moore, 2014, Antioxidants & redox signaling.

Bortezomib Warhead-Switch Confers Dual Activity against Mycobacterial Caseinolytic Protease and Proteasome and Selectivity against Human Proteasome

B. Dymock, T. Dick, Sridhar Santhanakrishnan, 2017, Front. Microbiol..

Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthr

J. Wood, A. Poulsen, A. William, 2012, Journal of medicinal chemistry.

3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.

X. Barril, M. Drysdale, P. Workman, 2005, Bioorganic & medicinal chemistry letters.

Overcoming chloroquine resistance in malaria: Design, synthesis and structure-activity relationships of novel chemoreversal agents.

F. Nosten, B. Dymock, K. Tan, 2016, European journal of medicinal chemistry.

Hydrogen Sulfide Promotes Adipogenesis in 3T3L1 Cells

P. Moore, B. Dymock, W. Feng, 2015, PloS one.

Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.

B. Dymock, Sabine Löbbe, M. Brewer, 2008, Bioorganic & medicinal chemistry letters.

Design and synthesis of triple inhibitors of janus kinase (JAK), histone deacetylase (HDAC) and Heat Shock Protein 90 (HSP90).

B. Dymock, Lianbin Yao, S. Ohlson, 2018, Bioorganic & medicinal chemistry letters.

2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.

Chang Kai Soh, Kay Lin Goh, Z. Bonday, 2012, Bioorganic & medicinal chemistry letters.

Novel Approaches to the Treatment of Hepatitis C Virus Infection

F. Wilson, B. Dymock, P. S. Jones, 2000, Antiviral chemistry & chemotherapy.

3-(Trimethylsilyl)oxetan-2-ones via enantioselective [2 + 2] cycloaddition of (trimethylsilyl)ketene to aldehydes catalysed by methylaluminiomidazolines

B. Dymock, P. Kocieňski, J. Pons, 1996 .

4-Amino derivatives of the Hsp90 inhibitor CCT018159.

Xavier Barril, Paul Workman, Allan M Jordan, 2006, Bioorganic & medicinal chemistry letters.

Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-

J. Wood, A. Poulsen, Meredith Williams, 2012, Journal of medicinal chemistry.

A Synthesis of the Hypocholesterolemic Agent 1233A Via Asymmetric [2 + 2] Cycloaddition

B. Dymock, P. Kocieňski, J. Pons, 1998 .

3‐(Trimethylsilyl)oxetan‐2‐ones via Enantioselective (2 + 2) Cycloaddition of (Trimethylsilyl)ketene to Aldehydes Catalyzed by Methylaluminoimidazolines.

B. Dymock, P. Kocieňski, J. Pons, 1996 .

Discovery of the cancer cell selective dual acting anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131).

Mayumi Kitagawa, B. Dymock, Sang Hyun Lee, 2018, European journal of medicinal chemistry.

DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: synthesis and antibacterial activity.

Paul N. Mortenson, L. Czaplewski, C. Smee, 2009, Bioorganic & medicinal chemistry letters.

Discovery of New H2S Releasing Phosphordithioates and 2,3-Dihydro-2-phenyl-2-sulfanylenebenzo[d][1,3,2]oxazaphospholes with Improved Antiproliferative Activity.

P. Moore, B. Dymock, Dejian Huang, 2015, Journal of medicinal chemistry.

GYY4137, a novel water-soluble, H2S-releasing molecule.

P. Moore, B. Dymock, P. Rose, 2015, Methods in enzymology.

NINE GYY 4137 , a Novel Water-Soluble , H 2 S-Releasing Molecule

P. Moore, B. Dymock, P. Rose, 2015 .

Novel squalestatin derivatives arising from reactions at the allylic centre of the C1-side chain

B. Dymock, P. Sidebottom, P. Procopiou, 1998 .

Overcoming Chloroquine Resistance in Malaria: Design, Synthesis, and Structure-Activity Relationships of Novel Hybrid Compounds

F. Nosten, B. Dymock, K. Tan, 2016, Antimicrobial Agents and Chemotherapy.

Identification of a novel class of orally active pyrimido[5,4-3][1,2,4]triazine-5,7-diamine-based hypoglycemic agents with protein tyrosine phosphatase inhibitory activity.

L. Setti, B. Dymock, F. Falcioni, 2003, Bioorganic & medicinal chemistry letters.

Inhibitors of HSP90 and other chaperones for the treatment of cancer

M. Drysdale, P. Workman, B. Dymock, 2004 .

Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.

S. Haider, B. Dymock, W. Chng, 2019, European journal of medicinal chemistry.

Selective JAK inhibitors.

B. Dymock, Lianbin Yao, Brian W Dymock, 2014, Future medicinal chemistry.

Intranasal administration of a stapled relaxin‐3 mimetic has anxiolytic‐ and antidepressant‐like activity in rats

R. Kini, A. Poulsen, B. Dymock, 2019, British journal of pharmacology.

Predicting chemotherapeutic drug combinations through gene network profiling

Brian Dymock, Edmund Jon Deoon Lee, Louxin Zhang, 2016, Scientific Reports.

A Small Molecule Targeting the Transmembrane Domain of Death Receptor p 75 NTR Induces Melanoma Cell Death and Reduces Tumor Growth Graphical

B. Dymock, B. Berger, C. Ibáñez, 2018 .

Discovery of Kinase Spectrum Selective Macrocycle

J. Wood, A. Poulsen, Meredith Williams, 2011 .

Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lympho

Anders Poulsen, Stéphanie Blanchard, Harish Nagaraj, 2011, Journal of medicinal chemistry.

Design and Synthesis of Ligand Efficient Dual Inhibitors of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Based on Ruxolitinib and Vorinostat.

J. Yen, A. Poulsen, B. Dymock, 2017, Journal of medicinal chemistry.

Recently discovered EZH2 and EHMT2 (G9a) inhibitors.

B. Dymock, Uttara Soumyanarayanan, 2016, Future medicinal chemistry.

New patented histone deacetylase inhibitors

Haishan Wang, B. Dymock, Brian W Dymock, 2009, Expert opinion on therapeutic patents.

The squalestatins: decarboxy and 4-deoxy analogues as potent squalene synthase inhibitors.

C. Chan, B. Dymock, J. Scicinski, 1996, Journal of medicinal chemistry.

Structure-based design of nitrogen-linked macrocyclic kinase inhibitors leading to the clinical candidate SB1317/TG02, a potent inhibitor of cyclin dependant kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3)

A. Poulsen, Meredith Williams, H. Nagaraj, 2012, Journal of Molecular Modeling.

Discovery of medium ring thiophosphorus based heterocycles as antiproliferative agents.

P. Moore, B. Dymock, W. Feng, 2017, Bioorganic & medicinal chemistry letters.

Hydrocarbon stapled B chain analogues of relaxin-3 retain biological activity

D. Herr, A. Poulsen, B. Dymock, 2016, Peptides.

Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.

Brian Dymock, Xavier Barril, Roderick E Hubbard, 2004, Bioorganic & medicinal chemistry letters.

Chemical Therapeutics VS-5584 , a Novel and Highly Selective PI 3 K / mTOR Kinase Inhibitor for the Treatment of Cancer

U. McDermott, M. Garnett, C. Benes, 2013 .

VS-5584, a Novel and Highly Selective PI3K/mTOR Kinase Inhibitor for the Treatment of Cancer

U. McDermott, M. Garnett, C. Benes, 2012, Molecular Cancer Therapeutics.

Dual blockade of the lipid kinase PIP4Ks and mitotic pathways leads to cancer-selective lethality

P. Nordlund, O. Sampetrean, H. Saya, 2017, Nature Communications.

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.

Design and synthesis of potent dual inhibitors of JAK2 and HDAC based on fusing the pharmacophores of XL019 and vorinostat.

J. Yen, A. Poulsen, B. Dymock, 2018, European journal of medicinal chemistry.

A novel slow-releasing hydrogen sulfide donor, FW1256, exerts anti-inflammatory effects in mouse macrophages and in vivo.

P. Moore, B. Dymock, W. Feng, 2016, Pharmacological research.

The rise of epigenetic drug discovery.

B. Dymock, 2016, Future medicinal chemistry.

Structure and Ligand-Based Design of mTOR and PI3-Kinase Inhibitors Leading to the Clinical Candidates VS-5584 (SB2343) and SB2602

Anders Poulsen, Stéphanie Blanchard, Angeline Lee, 2014, J. Chem. Inf. Model..

Towards Selective Mycobacterial ClpP1P2 Inhibitors with Reduced Activity against the Human Proteasome

A. Poulsen, B. Dymock, T. Dick, 2017, Antimicrobial Agents and Chemotherapy.

Fragment-Based Whole Cell Screen Delivers Hits against M. tuberculosis and Non-tuberculous Mycobacteria

B. Dymock, T. Dick, P. M. Ramanujulu, 2016, Front. Microbiol..

Intracellular Hyper-Acidification Potentiated by Hydrogen Sulfide Mediates Invasive and Therapy Resistant Cancer Cell Death

R. Huang, P. Moore, B. Dymock, 2017, Front. Pharmacol..

Fluorescent Probes for H2S Detection and Quantification.

B. Dymock, W. Feng, 2015, Handbook of experimental pharmacology.

Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6).

A. Poulsen, B. Dymock, Lianbin Yao, 2018, Bioorganic & medicinal chemistry letters.

A fluorescence polarization assay for inhibitors of Hsp90.

X. Barril, M. Drysdale, P. Workman, 2006, Analytical biochemistry.

Prodrugs of the cancer cell selective anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131) are orally efficacious in a mouse model of resistant colon cancer.

Mayumi Kitagawa, B. Dymock, Sang Hyun Lee, 2019, Bioorganic & medicinal chemistry letters.

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.

Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus kinase 2 (JAK2) and Fms-like tyrosine kinase-3 (FLT3)

Anders Poulsen, Anthony William, Stéphanie Blanchard, 2012, Journal of Computer-Aided Molecular Design.

Design and Characterization of Libraries of Molecular Fragments for Use in NMR Screening against Protein Targets

Brian Dymock, Xavier Barril, Fareed Aboul-Ela, 2004, J. Chem. Inf. Model..

SAHA and cisplatin sensitize gastric cancer cells to doxorubicin by induction of DNA damage, apoptosis and perturbation of AMPK‐mTOR signalling

Y. C. Long, B. Dymock, E. Lee, 2018, Experimental cell research.

TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties

J. Wood, A. William, B. Dymock, 2012, Leukemia.

SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies

A. Poulsen, A. William, B. Dymock, 2011, Leukemia.

Mutation of histone H3 serine 86 disrupts GATA factor Ams2 expression and precise chromosome segregation in fission yeast

B. Dymock, Zhe Yang, Bingbing Ren, 2015, Scientific Reports.

SB1518: A Potent and Orally Active JAK2 Inhibitor for the Treatment of Myeloproliferative Disorders.

Z. Bonday, J. Wood, J. Griffin, 2007 .

Structure-based design of PDK1 inhibitors.

Chang Kai Soh, A. Poulsen, Meredith Williams, 2012, Bioorganic & medicinal chemistry letters.

A Small Molecule Targeting the Transmembrane Domain of Death Receptor p75NTR Induces Melanoma Cell Death and Reduces Tumor Growth.

B. Dymock, B. Berger, C. Ibáñez, 2018, Cell chemical biology.

The squalestatins: inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C3-modified analogues.

B. Dymock, P. Procopiou, A. Craven, 1994, Journal of medicinal chemistry.

Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening.

Kay Lin Goh, Z. Bonday, J. Wood, 2012, Bioorganic & medicinal chemistry letters.

nonaene ( SB 1578 ) , a Potent Inhibitor of Janus Kinase 2 / Fms-LikeTyrosine Kinase-3 ( JAK 2 / FLT 3 ) for the Treatment of Rheumatoid Arthritis

Anders Poulsen, Harish Nagaraj, Evelyn Tan, 2012 .

Antioxidants inhibit neuronal toxicity in Parkinson's disease‐linked LRRK2

K. Lim, B. Dymock, D. Angeles, 2016, Annals of clinical and translational neurology.

SB1578, a Novel Inhibitor of JAK2, FLT3, and c-Fms for the Treatment of Rheumatoid Arthritis

J. Wood, A. William, B. Dymock, 2012, The Journal of Immunology.

Supporting Information: Discovery of the Macrocycle 11-(2-Pyrrolidin-1-yl- ethoxy)-14,19-dioxa-5,7,26-triaza- tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa- 1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a Potent Janus Kinase 2/Fms-LikeTyrosine Kinase-3 (JAK2/FLT3) Inhibitor for the Treatment o

Harish, J. Wood, Meredith Williams, 2011 .

VS-5584, a Novel and Highly Selective PI3K/mTOR Kinase Inhibitor for the Treatment of Cancer

U. McDermott, M. Garnett, C. Benes, 2012, Molecular Cancer Therapeutics.