Phosphoinositide-3-kinase
δ (PI3Kδ) is a critical regulator
of cell growth and transformation and has been explored as a therapeutic
target for a range of diseases. Through the exploration of the thienopyrimidine
scaffold, we have identified a ligand-efficient methylation that leads
to remarkable selectivity for PI3Kδ over the closely related
isoforms. Interrogation through the Free–Wilson analysis highlights
the innate selectivity the thienopyrimidine scaffold has for PI3Kδ
and provides a predictive model for the activity against the PI3K
isoforms.
Pentose
and hexose sugars are abundant constituents of waste biomass, making them
sustainable, chiral building blocks for organic synthesis. The demand for
chiral saturated heterocyclic rings from the pharmaceutical industry is
increasing as they provide well-defined three-dimensional frameworks that show
increased metabolic resistance. Through the formation of thioacetals, sugars may
be manipulated in their straight-chain form and dehydrated selectively under
basic conditions at C-2. This approach was applied to an array of sugars and
extended to the production of useful chiral THFs via further selective
dehydration reactions.
Pentose
and hexose sugars are abundant constituents of waste biomass, making them
sustainable, chiral building blocks for organic synthesis. The demand for
chiral saturated heterocyclic rings from the pharmaceutical industry is
increasing as they provide well-defined three-dimensional frameworks that show
increased metabolic resistance. Through the formation of thioacetals, sugars may
be manipulated in their straight-chain form and dehydrated selectively under
basic conditions at C-2. This approach was applied to an array of sugars and
extended to the production of useful chiral THFs via further selective
dehydration reactions.
Sugars
are abundant in waste biomass, making them sustainable chiral
building blocks for organic synthesis. The demand for chiral saturated
heterocyclic rings for pharmaceutical applications is increasing as
they provide well-defined three-dimensional frameworks that show increased
metabolic resistance. A range of sugar thioacetals can be dehydrated
selectively at C-2 under mild basic conditions, and the resulting
ketene thioacetals can be applied to the production of useful chiral
building blocks via further selective dehydration reactions.
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