Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110α inhibitors

Kendall, Jackie D.;Rewcastle, Gordon W.;Frédérick, Raphaël;Mawson, Claire;Shepherd, Peter R.;et.al.
(2007) Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology — Vol. 15, n° 24, p. 7677-7687 (2007)

Files

1-s2.pdf
  • Restricted Access
  • Adobe PDF
  • 613.66 KB
Request a copy

Details

Authors
  • Kendall, Jackie D.Auckland Cancer Society Research Centre, School of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1020, New Zealand
    Author
  • Rewcastle, Gordon W.Auckland Cancer Society Research Centre, School of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1020, New Zealand
    Author
  • Frédérick, Raphaëlorcid-logoUCLouvain
    Author
  • Mawson, ClaireAuckland Cancer Society Research Centre, School of Medical and Health Sciences, The University of Auckland, Private Bag 92019, Auckland 1020, New Zealand
    Author
  • Shepherd, Peter R.Maurice Wilkins Centre for Molecular Biodiscovery, The University of Auckland, Private Bag 92019, Auckland 1020, New Zealand
    Author
Show more
Abstract
A series of 2-methyl-5-nitrobenzenesulfonohydrazides were prepared and evaluated as inhibitors of PI3K. An isoquinoline derivative shows good selectivity for the p110α isoform over p110β and p110δ, and also demonstrates good in vitro activity in a cell proliferation assay. Molecular modelling provides a rationalisation for the observed SAR. © 2007 Elsevier Ltd. All rights reserved.
Affiliations

Citations

  • APA
  • Chicago
  • FWB

Kendall, J. D., Rewcastle, G. W., Frédérick, R., Mawson, C., Denny, W. A., Marshall, E. S., Baguley, B. C., Chaussade, C., Jackson, S. P., & Shepherd, P. R. (2007). Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110α inhibitors. Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, 15(24), 7677-7687. https://doi.org/10.1016/j.bmc.2007.08.062 (Original work published 2007)