Swen Hoelder

Summary

Affiliation: Institute of Cancer Research
Country: UK

Publications

  1. doi 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. doi 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)
    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
  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. doi 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 Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B
    Ludovic Drouin
    The Institute of Cancer Research, Division of Cancer Therapeutics, Cancer Research UK Cancer Therapeutics Unit, 15 Cotswold Road, Sutton, London SM2 5NG, U K
    J Med Chem 58:2553-9. 2015
  10. doi 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

Collaborators

  • Richard Bayliss
  • Nathan Brown
  • Oleg Fedorov
  • Stefan Knapp
  • Julian Blagg
  • Ian Collins
  • Spiros Linardopoulos
  • Keith Jones
  • Paul A Clarke
  • Florence I Raynaud
  • Andrew M Fry
  • Panagis Filippakopoulos
  • Vassilios Bavetsias
  • Antony W Oliver
  • Paolo Innocenti
  • Lewis R Vidler
  • Kathy Boxall
  • Daniel K Whelligan
  • Rob L M Van Montfort
  • G Wynne Aherne
  • Savade Solanki
  • Kwai Ming J Cheung
  • Corine Mas-Droux
  • Ludovic Drouin
  • Angela Hayes
  • Manjuan Liu
  • Hannah Woodward
  • Craig McAndrew
  • Rosemary Burke
  • Sebastien Naud
  • Isaac M Westwood
  • M Cris Silva-Santisteban
  • Laura Wylie
  • Caterina Barillari
  • Dawn Taylor
  • Douglas W Thomson
  • Cynthia Tallant
  • Lisa O'Fee
  • Martin Philpott
  • Wasim Akhtar
  • Apirat Chaikuad
  • Sally McGrath
  • Susanne Muller
  • Octovia Monteiro
  • Catherine Rogers
  • Amy Wood
  • Amir Faisal
  • Sarah Picaud
  • Vanessa Choi
  • Alan Henley
  • Peter Sheldrake
  • Berry Matijssen
  • Grace Mak
  • Suzanne A Eccles
  • Michael Tomsett
  • Michelle D Garrett
  • Sam Peacock
  • Elaine Barrie
  • Ross Baker
  • Amin Mirza
  • Jessica Schmitt
  • Sarah Martin
  • Mark Gurden
  • Butrus Atrash
  • Melanie Valenti
  • Alexis de Haven Brandon
  • Meirion Richards
  • Maura Westlake
  • Fiona Rowan
  • Tara Hardy
  • Sharon Yeoh
  • Lisa Pickard
  • Joanne E Baxter
  • Samantha Burns
  • Charles G Grummitt

Detail Information

Publications12

  1. doi 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. doi 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)
    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
    ....
  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. doi 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 Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B
    Ludovic Drouin
    The Institute of Cancer Research, Division of Cancer Therapeutics, Cancer Research UK Cancer Therapeutics Unit, 15 Cotswold Road, Sutton, London SM2 5NG, U K
    J Med Chem 58:2553-9. 2015
    ..13 represents an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo. ..
  10. doi 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...
  11. 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...
  12. 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
    ....