1396341-72-2Relevant academic research and scientific papers
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway
Bruce, Ian,Akhlaq, Mohammed,Bloomfield, Graham C.,Budd, Emma,Cox, Brian,Cuenoud, Bernard,Finan, Peter,Gedeck, Peter,Hatto, Julia,Hayler, Judy F.,Head, Denise,Keller, Thomas,Kirman, Louise,Leblanc, Catherine,Grand, Darren Le,McCarthy, Clive,O'Connor, Desmond,Owen, Charles,Oza, Mrinalini S.,Pilgrim, Gaynor,Press, Nicola E.,Sviridenko, Lilya,Whitehead, Lewis
scheme or table, p. 5445 - 5450 (2012/09/22)
Using 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.
