Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway

…, E Budd, B Cox, B Cuenoud, P Finan, P Gedeck…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 17 p. 5445 - 5450

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被引用次数: 19

摘要

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.