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2005
Oxocarboxylic acids and esters
Q 0460
The Identification and Optimization of 2,4-Diketobutyric Acids as Flap Endo1 Inhibitors. — Diketobutyric acids of type (III) generally can be obtained
01- 079 nuclease
in good overall yields by base-promoted Claisen condensation and subsequent saponification. A more attractive route, as in the case of heterocyclic diketobutyrates (VII),
involves, after Suzuki coupling, the addition of the dianion of a pyruvic acid equivalent
to an ester. Diketobutyric acid (IIIb) is an example of a sub-micromolar inhibitor of the
DNA repair protein FEN1, while (IIIa) reveals greater than 10-fold selectivity over the
highly related endonuclease XPG. Acids (VII) show moderate activity against FEN1
but are quite selective for XPG. — (TUMEY*, L. N.; et al.; Bioorg. Med. Chem. Lett.
14 (2004) 19, 4915-4918; Athersys, Inc., Cleveland, OH 44115, USA; Eng.) —
H. Hoennerscheid
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