Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway
2012; Elsevier BV; Volume: 22; Issue: 17 Linguagem: Inglês
10.1016/j.bmcl.2012.07.042
ISSN1464-3405
AutoresIan C. Bruce, Mohammed Shahid Akhlaq, Graham C. Bloomfield, Emma Budd, Brian J. Cox, Bernard Cuenoud, Peter M. Finan, Peter Gedeck, Julia Hatto, Judy Hayler, Denise Head, Thomas H. Keller, Louise Kirman, Catherine Leblanc, Darren Le Grand, Clive McCarthy, Desmond O’Connor, Charles Owen, Mrinalini S. Oza, Gaynor Pilgrim, Nicola E. Press, Lilya Sviridenko, Lewis Whitehead,
Tópico(s)Cancer Treatment and Pharmacology
ResumoUsing a parallel synthesis approach to target a non-conserved region of the PI3K catalytic domain a pan-PI3K inhibitor 1 was elaborated to provide alpha, delta and gamma isoform selective Class I PI3K inhibitors 21, 24, 26 and 27. The compounds had good cellular activity and were selective against protein kinases and other members of the PI3K superfamily including mTOR and DNA-PK.
Referência(s)