Small-molecules that covalently react with a human prolyl hydroxylase-towards activity modulation and substrate capture
We describe covalently binding modulators of the activity of human prolyl hydroxylase domain 2 (PHD2) and studies towards a strategy for photocapture of PHD2 substrates. Reversible active site binding of electrophile bearing compounds enables susbsequent covalent reaction with a lysine residue (K408) in the flexible C-terminal region of PHD2 to give a modified protein that retains catalytic activity.
Bush, Jacob T.,Le?niak, Robert K.,Yeh, Tzu-Lan,Belle, Roman,Kramer, Holger,Tumber, Anthony,Chowdhury, Rasheduzzaman,Flashman, Emily,Mecinovi?, Jasmin,Schofield, Christopher J.
p. 1020 - 1023
(2019/01/28)
A highly efficient strategy for the synthesis of 3-substituted salicylic acids by either directed ortho-lithiation or halogen-metal exchange of substituted mom protected phenols followed by carboxylation
A highly efficient synthesis of various 3-substituted salicylic acids is described starting from inexpensive starting materials and requiring no special apparatus.
Lau, Stephen Y.W.,Keay, Brian A.
p. 1541 - 1545
(2007/10/03)
Microwave-assisted rapid Claisen rearrarangement on solid phase
O-Allylsalicylic acids anchored to merrifield resin, are rapidly rearranged to the corresponding ortho-allylsalicylic acids in high yields for the first time under microwave irradiation.
Kumar,Anjaneyulu,Reddy,Yadav
p. 1129 - 1130
(2007/10/03)
2,3-Dihydro-7-benzofurancarboxylic Acids
The syntheses of a series of title compounds 1 a-f bearing methyl groups in the heterocyclic part were described.Depending on the substitution pattern the Claisen rearrangement (path A) or the methodology of directed lithiations (path B) were used as the
Stanetty, Peter,Koller, Herbert,Puerstinger, Gerhard
p. 883 - 891
(2007/10/02)
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