Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway
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.
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
p. 5445 - 5450
(2012/09/22)
IMIDAZOPYRIDAZINES AS PI3K LIPID KINASE INHIBITORS
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Page/Page column 62
(2008/12/05)
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