Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway
I Bruce, M Akhlaq, GC Bloomfield, E Budd… - Bioorganic & medicinal …, 2012 - Elsevier
Bioorganic & medicinal chemistry letters, 2012•Elsevier
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.
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.
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.
Elsevier