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4-Acylamino-6-arylfuro[2,3-d]pyrimidines: potent and selective glycogen synthase kinase-3 inhibitors.

Bioorganic & medicinal chemistry letters 2004 Aug 2; 14(15):3907-11

Link to PubMed abstract

Maeda Y Y, Nakano M M, Sato H H, Miyazaki Y Y, Schweiker S SL, Smith J JL, Truesdale A AT

Chemistry Department, Tsukuba Research Laboratories, GlaxoSmithKline K.K., Wadai 43, Tsukuba, Ibaraki 300-4247, Japan.

Modeling studies of a furo[2,3-d]pyrimidine GSK-3 hit compound 1 superimposed onto the X-ray crystal structure of a legacy pyrazolo[3,4-c]pyridazine GSK-3 inhibitor 2 led to the identification of 4-acylamino-6-arylfuro[2,3-d]pyrimidine template 3. Synthesis of analogues based on template 3 has resulted in a number of potent and selective GSK-3beta inhibitors. The most potent and selective compound was the m-pyridyl analogue 24.