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Brian Dymock – Full List of Publications

 

Peer reviewer for:

 

  • Journal of Medicinal Chemistry

  • Bioorganic and Medicinal Chemistry Letters

  • Bioorganic and Medicinal Chemistry

  • Future Medicinal Chemistry

  • Journal of Combinatorial Chemistry

  • Chem Med Chem

  • Expert Opinion in Therapeutic Patents

  • Drug Discovery Today

  • Journal of Developing Drugs

  • Journal of Hematology and Oncology

  • Marine Drugs

  • MedChem Communications

  • Tetrahedron Letters

 

Published Journal Manuscripts, Reviews, Editorials

 

  • T. T. T. Nguyen, J. K. K. Chua, K. S. Seah, S. H. Koo, J. Y. Yee, E. G. Yang, K. K. Lim, S. Y. W. Pang, A. Yuen, W. H. Ang, B. Dymock, E. J. D. Lee and E. S. Chen. “Predicting chemotherapeutic drug combinations through gene network profiling” Sci. Rep. - accepted

 

  • D Sharan, Priyankan, Dario C. Angeles, Patrick Ho, Brian W. Dymock, Kah-Leong Lim, and Eng-King Tan. "Antioxidant kinase inhibitors for LRRK2 Parkinson's disease." Parkinsonism & Related Disorders 22 (2016): e166-e167

 

  • K. T. Lim, T. Y. R. Ong, Y. R. Tan, E. G. Yang, B. Ren, K. S. Seah, Z. Yang, T. S. Tan, B. W. Dymock, and Ee Sin Chen. "Mutation of histone H3 serine 86 disrupts GATA factor Ams2 expression and precise chromosome segregation in fission yeast." Scientific reports 5 (2015), doi:10.1038/srep14064.

 

  • F. Wei, and B. W. Dymock. "Fluorescent Probes for H2S Detection and Quantification." In Chemistry, Biochemistry and Pharmacology of Hydrogen Sulfide, pp. 291-323. Springer International Publishing, 2015.

 

  • F., Wei, X-Y. Teo, W. Novera, P. M. Ramanujulu, D. Liang, D. Huang, P. K. Moore, L-W. Deng, and B. W. Dymock. "Discovery of new H2S releasing phosphordithioates and 2, 3-dihydro-2-phenyl-2-sulfanylenebenzo [d][1, 3, 2] oxazaphospholes with improved antiproliferative activity." Journal of medicinal chemistry 58, no. 16 (2015): 6456-6480.

 

  • P. Rose, B. W. Dymock, P. K. Moore, GYY4137, a novel water-soluble, H2S-releasing molecule, Methods in Enzymology, 2015; 554:143-67. doi: 10.1016/bs.mie.2014.11.014. Epub 2015 Jan 10.

 

  • Poulsen, A.; William, A. D.; Dymock, B. W. Designed Macrocyclic Kinase Inhibitors. In Macrocycles in Drug Discovery, Levin, J., Ed. Royal Society of Chemistry: Cambridge, UK, 2015; pp 141-205. (book chapter)

 

  • A. Poulsen, H. Nagaraj, A. Lee, S. Blanchard, C. K. Soh, D. Chen, C. Lee, Z. C. Xiong, H. Wang, S. Hart, K. C. Goh, B. Dymock, M. Williams Structure and ligand-based design of mTOR and PI3-kinase inhibitors leading to the clinical candidates VS-5584 (SB2343) and SB2602 J. Cheminf. Model. 2014 54(11):3238-50. doi: 10.1021/ci500493m. Epub 2014 Oct 23.

 

  • B. W. Dymock, E. G. Yang, J. Chu and L. Yao Selective JAK Inhibitors, Fut. Med. Chem., 2014, 6(12), 1439-1471.  DOI: 10.4155/fmc.14.92.

 

  • Liao, L.X., Tsai, C.Y., Atan, M.S., Lee, Z.W., Deng, L.W., Dymock, B.W., Feng, W., Tan, C-H., Moore, P.K. (2013). Identification of a novel slow releasing hydrogen sulfide donor for cancer therapy. Nitric Oxide, 31, Suppl 2:S47. doi: 10.1016/j.niox.2013.06.090.

 

  • B. Qabazard, L. Li, J. Gruber, M.T. Peh, L.F. Ng, K.S. Dinesh, P. Rose, C.H. Tan, B.W. Dymock, F. Wei, S.C. Swain, B. Halliwell, S.R. Stürzenbaum, P.K. Moore. Hydrogen Sulfide Is an Endogenous Regulator of Aging in Caenorhabditis elegans. Antioxid Redox Signal. 2014, Jun 1;20(16):2621-30. doi: 10.1089/ars.2013.5448. Epub 2013 Nov 21.

 

 

  • S. Hart, K.C. Goh, V. Novotny-Diermayr, M. Williams, Y. C. Tan, L. C. Ong, A. Cheong, B. K. Ng, H. Nagaraj, R. Jayaraman, K.M. Pasha, K. Ethirajulu, W.J. Chng, G.B. Cher, M.Garnett, U. McDermott, C. Benes, B. Dymock and J.M. Wood VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.  Mol. Cancer Ther., Mol Cancer Ther. 2013, 12(2),151-61.

 

  • Dymock, BW and See, CS, Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 – 2012, Expert Opin Ther Pat., 2013, 23(4), 449-501.   doi: 10.1517/13543776.2013.765862. Epub 2013 Feb 1

 

  • A. Poulsen, A. William, S. Blanchard, H. Nagaraj, M. Williams, H. Wang, A. Lee, E. Sun, E. Teo, E. Tan, K.C. Goh and B. Dymock. 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) J. Mol. Model., 2013, 19,119-30. DOI: 10.1007/s00894-012-1528-7.

 

  • B. Madan, K. Chuan Goh, S. Hart, A.D. William, R. Jayaraman, K. Ethirajulu, B.W. Dymock, J.M. Wood SB1578, a novel inhibitor of JAK2, FLT3, and c-Fms for the treatment of rheumatoid arthritis.J. Immunol. 2012,189(8):4123-34. DOI: 10.4049/jimmunol.1200675.

 

  • A.C.-H. Lee, M.S. Ramanujulu, D.M. Ma and B.W. Dymock  Thienopyrimidin-4-one derivatives as PDK1 inhibitors discovered through Fragment-based Screening. Bioorg. Med. Chem. Lett., 2012, 22, 4023-4027. DOI: 10.1016/j.bmcl.2012.04.080

     

  • A. Poulsen, A. William, S. Blanchard, A. Lee, H. Nagaraj, H. Wang, E. Teo, E. Tan, K.C. Goh and B. Dymock.  Structure-based design of oxygen-linked macrocyclic kinase inhibitors: discovery of SB1518 and SB1578, potent inhibitors of Janus Kinase 2 (JAK2) and Fms-LikeTyrosine Kinase-3 (FLT3) J. Comp. Aided Mol. Des., 2012, 26(4), 437-450. DOI: 10.1007/s10822-012-9572-z.

 

  • S. Blanchard, C.K. Soh, C.P. Lee, A. Poulsen, Z. Bonday, K.L. Goh, K.C. Goh, M.K. Goh, M.K. Pasha, H. Wang, M. Williams, J. Wood, K. Ethirajulu and B. Dymock. 2-Anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1 Bioorg. Med. Chem. Lett. 2012, 22(8), 2880-2884. Just Accepted Manuscript: DOI: 10.1016/j.bmcl.2012.02.058.

 

  • A. D. William, A.CH. Lee, A. Poulsen, K.C. Goh, B. Madan,S. Hart, E. Tan, H. Wang, H. Nagaraj, D. Chen, C.P. Lee, E.T. Sun, R. Jayaraman, M.K. Pasha, K. Ethirajulu, J.M. Wood, B.W. Dymock. 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-LikeTyrosine Kinase-3 (JAK2/FLT3) for the Treatment of Rheumatoid Arthritis J. Med. Chem. 2012, 55(6), 2623-2640. Just Accepted Manuscript: DOI: 10.1021/jm201454n

 

  • A. Poulsen, M. Williams, H.M. Nagaraj, A.D. William, H. Wang, C.K. Soh, Z.C. Xiong, B. W. Dymock. Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors Bioorg. Med. Chem. Lett. 2012, 22, 1009-1013.

 

  • A.D. William, A.C.-H. Lee, S. Blanchard, A. Poulsen, E. Teo, H. Nagaraj, E. Tan, K.C. Goh, S. Hart, R. Jayaraman, M.K. Pasha, K. Ethirajulu, J.M. Wood and B.W. Dymock. Discovery of the Macrocycle (16E)-14-Methyl-20-oxa-5,7,14,26-tetraaza-tetracyclo[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), a Potent Inhibitor of Cyclin Dependant Kinases (CDKs), Janus Kinase 2 (JAK2) and Fms-LikeTyrosine Kinase-3 (FLT3) J. Med. Chem. 2012,.55, 169-106. 

 

  • A. Poulsen, S. Blanchard, C.K. Soh, C.P. Lee, M. Williams, H. Wang, B.W Dymock. Structure-based design of selective PDK1 inhibitors. Bioorg. Med. Chem. Lett. 2012, 22, 305-307.

 

  • K.C. Goh, V. Novotny-Diermayr, S. Hart, L. C. Ong, Y. K. Loh, A. Cheong, Y.C. Tan, C. Hu, R. Jayaraman, A. William, K.H.  Ong, B.W. Dymock, K. Ethirajulu, F. Burrows, J.M. Wood. TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia 2012, 26, 236-243.

 

  • S Hart, KC Goh, V Novotny-Diermayr, CY Hu, H Hentze, YC Tan, B Madan, C Amalini, YK Loh, LC Ong, AD William, A Lee, A Poulsen, R Jayaraman, KH Ong, K Ethirajulu, B.W. Dymock and JW Wood SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies Leukemia, 2011, 25, 1751-1759.

 

  • H. Wang, N. Yu, D. Chen, K. Lee, P. L. Lye, J. Chang, W. Deng, M. Ng, T. Lu, M. L. Khoo, A. Poulsen, K. Sangthongpitag, X. Wu, C. Hu, K.C. Goh, X. Wang, L. Fang, K. L. Goh, H. H. Khng, S. K. Goh, T. Ng, W. C. Ong, Z. Bonday, P. Yeo, X. Liu, E. Goh, L. S. New, N. Tu, B. Ni, J. Wood, B.W. Dymock, M. Entzeroth, E. T Sun and K. Ethirajulu. 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. J. Med. Chem. 2011, 54, 4694-4720.

 

     ** Highly Cited Article Award, J Med Chem, Feb 2013**

     ** Selected for LeadDiscovery's DailyUpdates as being of special interest to the drug development sector.      http://www.leaddiscovery.co.uk/articles/21604762/ **                     

     ** Selected and evaluated by the Faculty of 1000 (F1000), which places this work in a library of the top 2% of published articles in biology & medicine, July 2011. **

 

  • A.D. William, A. Lee, S. Blanchard, A. Poulsen, E. Teo, H. Nagaraj, E. Tan, D. Chen, M. Williams, E. Sun, K.C. Goh, W. Ong, S.K. Goh, S. Hart, R. Jayaraman, R.; M.K. Pasha, K. Ethirajulu, J. Wood, B.W. Dymock. 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 of Myelofibrosis and Lymphoma. J. Med. Chem. 2011, 54, 4638-4658.

 

  • H. Wang, B.W. Dymock.  New patented histone deacetylase inhibitors.   SBIO Pte Ltd,  Singapore,  Singapore.    Expert Opinion on Therapeutic Patents  (2009),  19(12),  1727-1757. (Review Article)

 

     ** Breakthrough work in Fragments to discover a new series of HSP90 inhibitors**

 

  • P.A. Brough, X. Barril, J. Borgognoni, P. Chene, N.G.M. Davies, B. Davis, M.J. Drysdale, B.W. Dymock, S.A. Eccles, C. Garcia-Echeverria, C. Fromont, A. Hayes, R.E. Hubbard, A.M. Jordan, M.R. Jensen, A. Massey, A. Merrett, A. Padfield, R. Parsons, T. Radimerski, F.I. Raynaud, A. Robertson, S.D. Roughley, J. Schoepfer, H. Simmonite, S.Y. Sharp, A. Surgenor, M. Valenti, S. Walls, P. Webb, M. Wood, P. Workman, L. Wright. 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. J. Med. Chem. 2009, 52, 4794-4809. 

 

  • East SP, White CB, Barker O, Barker S, Bennett J, Brown D, Boyd EA, Brennan C, Chowdhury C, Collins I, Convers-Reignier E, Dymock BW, Fletcher R, Haydon DJ, Gardiner M, Hatcher S, Ingram P, Lancett P, Mortenson P, Papadopoulos K, Smee C, Thomaides-Brears HB, Tye H, Workman J, Czaplewski LG. DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: synthesis and antibacterial activity.  Bioorg Med Chem Lett. 2009, 19 (3):894-9.

 

  • Eccles SA, Massey A, Raynaud FI, Sharp SY, Box G, Valenti M, Patterson L, de Haven Brandon A, Gowan S, Boxall F, Aherne W, Rowlands M, Hayes A, Martins V, Urban F, Boxall K, Prodromou C, Pearl L, James K, Matthews TP, Cheung KM, Kalusa A, Jones K, McDonald E, Barril X, Brough PA, Cansfield JE, Dymock B, Drysdale MJ, Finch H, Howes R, Hubbard RE, Surgenor A, Webb P, Wood M, Wright L, Workman P. NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. Cancer Res. 2008, 68 (8), 2850-60.

 

  • Ermann M, Riether D, Walker ER, Mushi IF, Jenkins JE, Noya-Marino B, Brewer ML, Taylor MG, Amouzegh P, East SP, Dymock BW, Gemkow MJ, Kahrs AF, Ebneth A, Löbbe S, O'Shea K, Shih DT, Thomson D. Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity. Bioorg Med Chem Lett. 2008, 18 (5):1725-9.

 

      ** Describes final med chem. story towards AUY922, now in Phase 2 with Novartis**

 

  • Paul A. Brough, Wynne Aherne, Xavier Barril, Jenifer Borgognoni, Kathy Boxall, Julie E. Cansfield, Kwai-Ming J. Cheung, Ian Collins, Nicholas G. M. Davies, Martin J. Drysdale, Brian Dymock, Suzanne A. Eccles, Harry Finch, Alexandra Fink, Angela Hayes, Robert Howes, Roderick E. Hubbard, Karen James, Allan M. Jordan, Andrea Lockie, Vanessa Martins, Andrew Massey, Thomas P. Matthews, Edward McDonald, Christopher J. Northfield, Laurence H. Pearl, Chrisostomos Prodromou, Stuart Ray, Florence I. Raynaud, Stephen D. Roughley, Swee Y. Sharp, Allan Surgenor, D. Lee Walmsley, Paul Webb, Mike Wood, Paul Workman and Lisa Wright, 4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer. J. Med. Chem., 2008, 51 (2), pp 196–218.

 

  • Sharp SY, Prodromou C, Boxall K, Powers MV, Holmes JL, Box G, Matthews TP, Cheung KM, Kalusa A, James K, Hayes A, Hardcastle A, Dymock B, Brough PA, Barril X, Cansfield JE, Wright L, Surgenor A, Foloppe N, Hubbard RE, Aherne W, Pearl L, Jones K, McDonald E, Raynaud F, Eccles S, Drysdale M, Workman P. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther. 2007 Apr;6(4):1198-211.

 

  • Smith NF, Hayes A, James K, Nutley BP, McDonald E, Henley A, Dymock B, Drysdale MJ, Raynaud FI, Workman P. Preclinical pharmacokinetics and metabolism of a novel diaryl pyrazole resorcinol series of heat shock protein 90 inhibitors. Mol Cancer Ther. 2006, 5 (6), 1628-37.

 

  • Barril, X.; Beswick, M.; Collier, A.; Drysdale, M.; Dymock, B. W.; Fink, A.; Grant, K.; Howes, R.; Jordan, A. M.; Massey, A.; Surgenor, A.; Wayne, J.; Workman, P. and Wright, L. 4-Amino derivatives of the Hsp90 inhibitor CCT018159, Bioorg. Med. Chem. Lett., 2006, 16 (9),  2543-2548

 

  • Howes, R.; Barril, X.; Dymock, B. W.; Grant, K.; Northfield, C. J.; Robertson, A. G. S.; Surgenor, A.; Wayne, J.; Wright, L.; James, K.; Matthews, T.; Cheung, K.-M.; McDonald, E.; Workman, P.; Drysdale, M. J.  A fluorescence polarization assay for inhibitors of Hsp90.    Analytical Biochemistry 2006, 350( 2),  202-213.

 

  • Brough, P. A.; Barril, X.; Beswick, M.; Dymock, B. W.; Drysdale, M. J.; Wright, L.; Grant, K.; Massey, A.; Surgenor, A.; Workman, P.  3-(5-chloro-2, 4-dihydroxyphenyl)-Pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone Bioorg. Med. Chem. Lett., 2005, 15, 5197-5201.

 

  • Dymock, Brian. SCIpharm: screen to candidate: new technology is improving pre-clinical drug discovery. Chemistry & Industry (London, United Kingdom)  (2005), (20),  26-27.

 

      ** Among most cited papers 2005 **

 

  • Dymock, B. W.; Barril, X.; Brough, P. A.; Cansfield, J. E.; Massey, A.; McDonald, E.; Hubbard, R. E.; Surgenor, A.; Roughley, S. D.; Webb, P.; Workman, P.; Wright, L.; Drysdale, M. J.; Novel, Potent Small-Molecule Inhibitors of the Molecular Chaperone Hsp90 Discovered through Structure-Based Design J. Med. Chem.; 2005; 48( 13); 4212-4215.

 

  • Baurin, N.; Aboul-Ela, F.; Barril, X.; Davis, B.; Drysdale, M.; Dymock, B.; Finch, H.; Fromont, C.; Richardson, C.; Simmonite, H.; Hubbard, R. E.; Design and Characterization of Libraries of Molecular Fragments for Use in NMR Screening against Protein Targets  J. Chem. Inf. Comput. Sci.; 2004; 44 (6); 2157-2166.

 

  • Dymock, B. W.; Drysdale, M. J.; MacDonald, E.; Workman, P. Inhibitors of Hsp90 and Other Chaperones for the Treatment of Cancer. Expert Opin. Ther. Pat. 2004, 14, 837-847. (Review Article)

 

  • Wright, L.; Barril, X.; Dymock, B.; Surgenor, A.; Beswick, M.; Drysdale, M.; Collier, A.; Massey, A.; Davies, N.; Fink, A.; Fromont, C.; Aherne, W.; Boxall, K.; Sharp, S.; Workman, P.; Hubbard, R. E. Structure-activity relationships in purine-based inhibitor binding to Hsp90 isoforms. Chem. Biol. 2004, 11, 775- 785.

 

  • Dymock, Brian W.; Drysdale, Martin J.; McDonald, Edward; Workman, Paul.  Inhibitors of HSP90 and other chaperones for the treatment of cancer. Expert Opinion on Therapeutic Patents 2004, 14 (6), 837-847. (Review Article)

 

       **Most cited paper 2003-2006 Award**

 

  • Dymock, B.; Barril, X.; Beswick, M.; Collier, A.; Davies, N.; Drysdale, M.; Fink, A.; Fromont, C.; Hubbard, R. E.; Massey, A.; Surgenor, A.; Wright, L. Adenine derived inhibitors of the molecular chaperone Hsp90-SAR explained through multiple X-ray structures. Bioorg. Med. Chem. Lett. 2004, 14, 325-328.

 

  • Guertin, Kevin R.; Setti, Lina; Qi, Lida; Dunsdon, Rachel M.; Dymock, Brian W.; Jones, Philip S.; Overton, Hilary; Taylor, Mathew; Williams, Glyn; Sergi, Joseph A.; Wang, Karen; Peng, Ying; Renzetti, Marcia; Boyce, Rogely; Falcioni, Fiorenza; Garippa, Ralph; Olivier, Andree R.  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. Bioorganic & Medicinal Chemistry Letters 2003, 13 (17), 2895-2898.

 

  • Dymock, B.W. Emerging Therapies for Hepatits C Virus Infection Emerging Drugs, 2001, 6, 13-42. (Review Article)

 

  • Dymock, B.W.; Jones, P.S. and Wilson, F.X. Novel Approaches to the Treatment of Hepatitis C Virus Infection Antiviral Chemistry and Chemotherapy, 2000, 11, 79-96. (Review Article)

 

  • Adelbrecht, J-C.; Craig, D.;Dymock, B.W.; Thorimbert, S. Synthesis of Hydroxypiperidines using 1,4-ditosytetrahydropyridines SynLett 2000, 467-470

 

  • Dymock, B.W.; Kocienski, P.J.; Pons, J-M. A Synthesis of the Hypocholesterolemic Agent 1233A via Asymmetric [2+2] Cycloaddition Synthesis, 1998, 1655-1661

 

  • Procopiou, Panayiotis A.; Dymock, Brian W.; Inglis, Graham G. A.; Lester, Michael G.; Roberts, Andrew D.; Sidebottom, Philip J.; Spooner, Stephen J.; Srikantha, Anton R. P.; Watson, Nigel S.  Novel squalestatin derivatives arising from reactions at the allylic center of the C1-side chain. Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry  1998, (2), 327-334.

 

  • Dymock, Brian W.; Kocienski, Philip J.; Pons, Jean-Marc.   3-(Trimethylsilyl)oxetan-2-ones via enantioselective [2+2] cycloaddition of (trimethylsilyl)ketene to aldehydes catalyzed by methylaluminoimidazolines. Chemical Communications (Cambridge)  1996, (9), 1053-1054. 

 

  • Chan, Chuen; Andreotti, Daniele; Cox, Brian; Dymock, Brian W.; Hutson, Julie L.; Keeling, Suzanne E.; McCarthy, Alun D.; Procopiou, Panayiotis A.; Ross, Barry C.; et al.  The Squalestatins: Decarboxy and 4-Deoxy Analogs as Potent Squalene Synthase Inhibitors. Journal of Medicinal Chemistry  1996, 39(1), 207-16.

 

  • Bamford, Mark J.; Chan, Chuen; Craven, Andrew P.; Dymock, Brian W.; Green, Darren; Henson, Richard A.; Kirk, Barrie E.; Lester, Michael G.; Procopiou, Panayiotis A.; et al.   The Squalestatins: Synthesis and Biological Activity of Some C3-Modified Analogs; Replacement of a Carboxylic Acid or Methyl Ester with an Isoelectronic Heterocyclic Functionality.    Journal of Medicinal Chemistry  1995, 38 (18), 3502-13.

 

  • Procopiou, Panayiotis A.; Bailey, Esme J.; Bamford, Mark J.; Craven, Andy P.; Dymock, Brian W.; Houston, John G.; Hutson, Julie L.; Kirk, Barrie E.; McCarthy, Alun D.; et al.   The Squalestatins: Novel Inhibitors of Squalene Synthase. Enzyme Inhibitory Activities and in vivo Evaluation of C1-Modified Analogs.    Journal of Medicinal Chemistry  1994, 37 (20), 3274-81.

 

Patent Publications

 

  • Robert K Mansfield, Tracy Lawhon, Brian Dymock. Solid State Forms of Macrocyclic Kinase Inhibitors. PCT Int. Appl. (2011), WO2011/097525.

    ​​Dymock, Brian; Lee, Cheng Hsia Angeline; William, Anthony Deodaunia. 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),2,4,9,14,16,18(26),20,22-nonaene citrate. PCT Int. Appl.  (2011), WO201100817.

 

  • Dymock, Brian; Lee, Cheng Hsia Angeline; William, Anthony Deodaunia 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 maleate salt. PCT Int. Appl. (2010), WO2010068182.

 

  • Dymock, Brian; Lee, Cheng Hsia Angeline; William, Anthony Deodaunia 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 citrate salt. PCT Int. Appl. (2010), WO2010068181.

 

  • Drysdale, Martin James; Dymock, Brian William; Krell, Christoph; Mutz, Michael; Petersen, Holger; Zheng, Weijia.   Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-yl-methyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms for treatment of Hsp90-mediated disorders. PCT Int. Appl. (2008), WO2008104595.

 

  • Drysdale, M. J.; Dymock, B. W.; Barril-Alonso, X. Use of pyrido[2,3-b]thiophene compounds as Hsp90 inhibitors – useful for the treatment of cancer or inflammatory diseases. PCT Int. Appl. (2005) WO05034950,

 

  • Dymock, B. W.; Drysdale, M. J.; Fromont, C.; Jordan, A.. New pyrimidothiophene derivatives are inhibitors of Hsp90– useful for immunosuppression or the treatment of viral infections and inflammation  PCT Int. Appl. (2005) WO05021552

 

  • Cheung, K. M.; Dymock, B. W.; MacDonald, E.; Drysdale, M. J. New substituted 5-membered cyclic derivatives are Hsp90 inhibitors – useful for the treatment of cancer or inflammatory diseases. PCT Int. Appl. (2005) WO05000300.

 

  • Barril-Alonso, Xavier; Dymock, Brian William; Drysdale, Martin James. Preparation of amino acid pyrazolecarboxamides as heat shock protein 90 (HSP90) inhibitors for the treatment of cancer. PCT Int. Appl. (2004), WO2004096212

 

  • Dunn, James Patrick; Dymock, Brian William; Mirzadegan, Taraneh; Sjogren, Eric Brian; Swallow, Steven; Sweeney, Zachary Kevin.   Preparation of benzyl-pyridazinones as reverse transcriptase inhibitors. PCT Int. Appl. (2004), WO2004085406

 

  • Drysdale, Martin James; Dymock, Brian William; Finch, Harry; Webb, Paul; Mcdonald, Edward; James, Karen Elizabeth; Cheung, Kwai Ming; Mathews, Thomas Peter.  Isoxazole compounds as inhibitors of heat shock proteins  PCT Int. Appl. (2004), WO04072051

 

  • Beswick, Mandy Christine; Drysdale, Martin James; Dymock, Brian William; Mcdonald, Edward; Pyrazole compounds. PCT Int. Appl. (2004), WO2004056782

 

  • Beswick, Mandy Christine; Brough, Paul Andrew; Drysdale, Martin James; Dymock, Brian William. Preparation of 3-(2-hydroxyphenyl)-1H-pyrazole-4-carboxamides as HSP90 inhibitors for the treatment of cancer. PCT Int. Appl. (2004), WO2004050087.

 

  • Drysdale, M. J.; Dymock, B. W.; Barril-Alonso, X.; Workman, P.; Pearl, L. H.; Prodromou, C.; MacDonald, E. Preparation of 3,4-diarylpyrazoles as inhibitors of heat shock protein 90 (Hsp90) and their use in the therapy of cancer. PCT Int. Appl. (2003) WO03055860.

 

  • Dymock, Brian William; Gill, Adrian Liam; Jones, Philip Stephen; Parkes, Kevin Edward Burdon; Parratt, Martin John. Preparation of pyrazoles as HIV reverse transcriptase inhibitors. PCT Int. Appl. (2002), WO2002100853.

 

  • Dymock, Brian William; Jones, Philip Stephen; Merrett, John Herbert; Parkes, Kevin Edward Burdon; Parratt, Martin John; Walter, Daryl Simon.  Preparation of imidazolones for the treatment of viral diseases. PCT Int. Appl.  (2002), WO0242279.

 

  • Dymock, Brian William; Jones, Philip Stephen; Merrett, John Herbert; Parratt, Martin John.  Preparation of pyrazoles for the treatment of viral diseases  PCT Int. Appl. (2002), WO0230907.

 

  • Devos, Rene; Dymock, Brian William; Hobbs, Christopher John; Jiang, Wen-rong; Martin, Joseph Armstrong; Merrett, John Herbert; Najera, Isabel; Shimma, Nobuo; Tsukuda, Takuo.  Preparation of antiviral nucleoside derivatives as inhibitors of subgenomic hepatitis C virus RNA replication  PCT Int. Appl. (2002), WO0218404.

 

  • Dymock, Brian William; Jones, Philip Stephen; Merrett, John Herbert; Parratt, Martin John.  Preparation of pyrrole derivatives for treating AIDS  PCT Int. Appl.  (2002), WO  0202524

 

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