Swen Hoelder

Summary

Affiliation: Institute of Cancer Research
Country: UK

Publications

  1. ncbi Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines
    Paolo Innocenti
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Belmont, Surrey, SM2 5NG, UK
    Org Biomol Chem 13:893-904. 2015
  2. pmc Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization
    Daniel K Whelligan
    Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 53:7682-98. 2010
  3. pmc Discovery of small molecule cancer drugs: successes, challenges and opportunities
    Swen Hoelder
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Mol Oncol 6:155-76. 2012
  4. ncbi Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship
    Savade Solanki
    The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 54:1626-39. 2011
  5. pmc Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening
    Lewis R Vidler
    Division of Cancer Therapeutics, Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 56:8073-88. 2013
  6. pmc Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)
    Sébastien 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
  7. pmc Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2
    M Cris Silva-Santisteban
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom
    PLoS ONE 8:e65689. 2013
  8. ncbi Two-step synthesis of aza- and diazaindoles from chloroamino-N-heterocycles using ethoxyvinylborolane
    Daniel K Whelligan
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    J Org Chem 75:11-5. 2010
  9. pmc Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
    Lewis R Vidler
    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 55:7346-59. 2012
  10. pmc Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity
    Paolo Innocenti
    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 55:3228-41. 2012

Collaborators

Detail Information

Publications11

  1. ncbi Expanding the scope of fused pyrimidines as kinase inhibitor scaffolds: synthesis and modification of pyrido[3,4-d]pyrimidines
    Paolo Innocenti
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, 15 Cotswold Road, Belmont, Surrey, SM2 5NG, UK
    Org Biomol Chem 13:893-904. 2015
    ..Our strategy involves the concise preparation of 8-chloro-2-(methylthio)pyrido[3,4-d]pyrimidine intermediates and their efficient derivatisation to give novel compounds with potential as kinase inhibitors. ..
  2. pmc Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization
    Daniel K Whelligan
    Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 53:7682-98. 2010
    ..The implications of these observations are discussed, and the work described here defines key features for potent and selective Nek2 inhibition, which will aid the identification of more advanced inhibitors of Nek2...
  3. pmc Discovery of small molecule cancer drugs: successes, challenges and opportunities
    Swen Hoelder
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    Mol Oncol 6:155-76. 2012
    ..We envisage a future in which addressing these challenges will enhance our rapid progress towards truly personalised medicine for cancer patients...
  4. ncbi Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship
    Savade Solanki
    The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 54:1626-39. 2011
    ..These observations were further investigated, and structure-based design led to Nek2 inhibitors derived from (R)-1 with more than a hundred-fold selectivity against Plk1...
  5. pmc Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening
    Lewis R Vidler
    Division of Cancer Therapeutics, Cancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, 15 Cotswold Road, Sutton, Surrey SM2 5NG, United Kingdom
    J Med Chem 56:8073-88. 2013
    ..This work provides a validated virtual screening approach that is applicable to other BRDs and describes novel KAc mimetics that can be further explored to design more potent inhibitors. ..
  6. pmc Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)
    Sébastien 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
    ....
  7. pmc Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2
    M Cris Silva-Santisteban
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, Sutton, Surrey, United Kingdom
    PLoS ONE 8:e65689. 2013
    ....
  8. ncbi Two-step synthesis of aza- and diazaindoles from chloroamino-N-heterocycles using ethoxyvinylborolane
    Daniel K Whelligan
    Cancer Research UK Centre for Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK
    J Org Chem 75:11-5. 2010
    ..The method involves an optimized Suzuki-Miyaura coupling with (2-ethoxyvinyl)borolane followed by acetic acid-catalyzed cyclization...
  9. pmc Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites
    Lewis R Vidler
    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 55:7346-59. 2012
    ....
  10. pmc Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2: structure-activity relationship, structural biology, and cellular activity
    Paolo Innocenti
    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 55:3228-41. 2012
    ..These compounds have been designed by combining key elements of two previously discovered chemical series. Structure based design led to aminopyridine (R)-21, a potent and selective inhibitor able to modulate Nek2 activity in cells...
  11. ncbi Synthesis of amino-substituted indoles using the Bartoli reaction
    Laura Wylie
    Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, Haddow Laboratories, 15 Cotswold Road, Sutton, Surrey, SM2 5NG, UK
    Org Biomol Chem 10:4441-7. 2012
    ..Our work thus represents a novel entry into substituted aminoindoles which are relevant building blocks for both the fine chemical and pharmaceutical industry...