Vassilios Bavetsias

Summary

Affiliation: Institute of Cancer Research
Country: UK

Publications

  1. ncbi request reprint Targeting the alpha-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase
    Elisa A Henderson
    Department of Chemistry, Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, Cancer Research Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Bioorg Med Chem 14:5020-42. 2006
  2. pmc Assessing histone demethylase inhibitors in cells: lessons learned.
    Stephanie B Hatch
    Epigenetics Chromatin 10:9. 2017
  3. pmc 7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, United Kingdom Electronic address
    Bioorg Med Chem Lett 25:4203-9. 2015
  4. doi request reprint Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate
    Vassilios Bavetsias
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, United Kingdom
    J Med Chem 53:5213-28. 2010
  5. ncbi request reprint Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases
    Vassilios Bavetsias
    Department of Chemistry, Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK Laboratory, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Bioorg Med Chem Lett 17:6567-71. 2007
  6. pmc The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo
    Amir Faisal
    Cancer Research UK, Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, SM2 5NG, United Kingdom
    Mol Cancer Ther 10:2115-23. 2011
  7. pmc Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 55:8721-34. 2012
  8. ncbi request reprint Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity
    Florence Chan
    Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK, 15 Cotswold Road, Belmont, Surrey SM2 5NG, United Kingdom
    Mol Cancer Ther 6:3147-57. 2007
  9. pmc Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom
    J Med Chem 56:9122-35. 2013
  10. doi request reprint Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells
    Nathalie Bouloc
    Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, Sutton, Surrey, United Kingdom
    Bioorg Med Chem Lett 20:5988-93. 2010

Collaborators

Detail Information

Publications22

  1. ncbi request reprint Targeting the alpha-folate receptor with cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase
    Elisa A Henderson
    Department of Chemistry, Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, Cancer Research Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Bioorg Med Chem 14:5020-42. 2006
    ..Compound 2b (2-CH2OH derivative) displayed the highest selectivity for the A431-FBP cells compared with A431 cells...
  2. pmc Assessing histone demethylase inhibitors in cells: lessons learned.
    Stephanie B Hatch
    Epigenetics Chromatin 10:9. 2017
    ..In addition, the presented data may inform further studies to assess the cell-based activity of histone lysine methylation inhibitors...
  3. pmc 7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research, London, United Kingdom Electronic address
    Bioorg Med Chem Lett 25:4203-9. 2015
    ..Compounds 7a and 14d interact with the P-loop whereas 14a and 14b engage with Thr217 in the post-hinge region. These crystallographic insights provide options for the design of compounds interacting with the DFG motif or with Thr217. ..
  4. doi request reprint Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate
    Vassilios Bavetsias
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, United Kingdom
    J Med Chem 53:5213-28. 2010
    ..019 muM). Compound 51 is highly orally bioavailable, and in in vivo efficacy studies it inhibited the growth of SW620 colon carcinoma xenografts following oral administration with no observed toxicities as defined by body weight loss...
  5. ncbi request reprint Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases
    Vassilios Bavetsias
    Department of Chemistry, Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK Laboratory, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Bioorg Med Chem Lett 17:6567-71. 2007
    ..042, 0.198 and 0.227microM, respectively. Compound 31 inhibits cell proliferation and has good microsomal stability...
  6. pmc The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo
    Amir Faisal
    Cancer Research UK, Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, SM2 5NG, United Kingdom
    Mol Cancer Ther 10:2115-23. 2011
    ..The potent preclinical activity of CCT137690 suggests that this inhibitor may benefit patients with MYCN-amplified neuroblastoma...
  7. pmc Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 55:8721-34. 2012
    ..Compound 27e, an orally bioavailable dual FLT3 and Aurora kinase inhibitor, was selected as a preclinical development candidate for the treatment of human malignancies, in particular AML, in adults and children...
  8. ncbi request reprint Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity
    Florence Chan
    Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK, 15 Cotswold Road, Belmont, Surrey SM2 5NG, United Kingdom
    Mol Cancer Ther 6:3147-57. 2007
    ..This has facilitated the use of 3'-deoxy-3'[(18)F]fluorothymidine-positron emission tomography to measure noninvasively the biological activity of the Aurora kinase inhibitor CCT129202 in vivo...
  9. pmc Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom
    J Med Chem 56:9122-35. 2013
    ..These compounds are useful small-molecule chemical tools to further explore the function of Aurora-A in cells. ..
  10. doi request reprint Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells
    Nathalie Bouloc
    Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, Sutton, Surrey, United Kingdom
    Bioorg Med Chem Lett 20:5988-93. 2010
    ..This led to the design and synthesis of potent Aurora-A inhibitors demonstrating up to 70-fold selectivity in cell-based Aurora kinase pharmacodynamic biomarker assays...
  11. doi request reprint Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs)
    Stephen Gorsuch
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Cancer Research UK Laboratories, Cotswold Road, Sutton, Surrey, SM2 5NG, UK
    Bioorg Med Chem 17:467-74. 2009
    ..1 microM) to encourage further exploration of this bicyclic structure. The foregoing SAR is consistent with an inhibitory mechanism involving cleavage of the S-N bond of the isothiazolone ring by a catalytically important thiol residue...
  12. pmc Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)
    Sebastien Naud
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London SM2 5NG, United Kingdom
    J Med Chem 56:10045-65. 2013
    ....
  13. pmc Pyrido[3,4-d]pyrimidin-4(3H)-one metabolism mediated by aldehyde oxidase is blocked by C2-substitution
    Angela Hayes
    a Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London, UK
    Xenobiotica . 2016
    ..4. In addition to the experimental data, these observations are supported by molecular modelling studies in the human AO protein crystal structure...
  14. ncbi request reprint Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B
    Ian Collins
    Cancer Research, UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton, Surrey
    Bioorg Med Chem 14:1255-73. 2006
    ..Potent PKB inhibitors from this series inhibited GSK3beta phosphorylation in cellular assays, consistent with inhibition of PKB kinase activity in cells...
  15. doi request reprint Regioselective C2-arylation of imidazo[4,5-b]pyridines
    Jonathan MacDonald
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey SM2 5NG, UK
    Org Biomol Chem 11:2335-47. 2013
    ..Mechanistic observations are consistent with a concerted-metallation-deprotonation mechanism facilitated by coordination of copper(I)iodide to the imidazo[4,5-b]pyridine...
  16. ncbi request reprint BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors
    David D Gibbs
    Section of Medicine and Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Sutton
    Cancer Res 65:11721-8. 2005
    ..5- and 4.6-fold, respectively). These data suggest that BGC 945 selectively inhibits thymidylate synthase in alpha-FR-overexpressing tumors and should cause minimal toxicity to humans at therapeutic doses...
  17. ncbi request reprint Antifolate chemistry: synthesis of 4-[N-[(6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl]-N-(prop-2-ynyl)amino]benzoic acid via a (propargyl)Co2(CO)6+ complex
    Vassilios Bavetsias
    Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, Chemistry Department, Cancer Research UK Laboratory, 15 Cotswold Road, Sutton, Surrey, UK SM2 5NG
    Org Biomol Chem 1:1943-6. 2003
    ....
  18. ncbi request reprint Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity
    Lindsay Stimson
    Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    Mol Cancer Ther 4:1521-32. 2005
    ..As one of the first series of small-molecule inhibitors of HAT activity, further analogue synthesis is being pursued to examine the potential scope for reducing chemical reactivity while maintaining HAT inhibition...
  19. pmc 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
    Vassilios Bavetsias
    Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, London SM2 5NG, U K
    J Med Chem 59:1388-409. 2016
    ....
  20. doi request reprint ClTi(OiPr)3-promoted reductive amination on the solid phase: combinatorial synthesis of a biaryl-based sulfonamide library
    Corey D Gutierrez
    Cancer Research UK Centre for Cancer Therapeutics at The Institute of Cancer Research, Cancer Research UK, Laboratory, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Comb Chem 10:280-4. 2008
    ..The library members were obtained in moderate quantity (1-8 mg) with over 70% of the sampled products greater than 90% pure according to LC-MS analysis...
  21. ncbi request reprint Selective delivery of CB300638, a cyclopenta[g]quinazoline-based thymidylate synthase inhibitor into human tumor cell lines overexpressing the alpha-isoform of the folate receptor
    Davinder S Theti
    Section of Medicine, The Institute of Cancer Research, Sutton, Surrey, SM2 5NG, United Kingdom
    Cancer Res 63:3612-8. 2003
    ....
  22. ncbi request reprint Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation
    Rosanna Sorrentino
    Dipartimento di Biologia e Patologia Cellulare e Molecolare, Universita Federico II, Via S Pansini 5, 80131 Napoli, Italy
    J Clin Endocrinol Metab 90:928-35. 2005
    ..The block of Aurora B expression induced by RNA interference or by using an inhibitor of Aurora kinase activity significantly reduced the growth of thyroid anaplastic carcinoma cells...