Synthesis of purin-2-yl and purin-6-yl-aminoglucitols as C-nucleosidic ATP mimics and biological evaluation as FGFR3 inhibitors

L Tak-Tak, F Barbault, F Maurel, P Busca…

Index: Tak-Tak, Lotfi; Barbault, Florent; Maurel, Franois; Busca, Patricia; Le Merrer, Yves European Journal of Medicinal Chemistry, 2011 , vol. 46, # 4 p. 1254 - 1262

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Citation Number: 4

Abstract

Two new series of C-nucleosidic ATP mimics have been synthesized using an efficient and versatile synthetic pathway. These compounds were designed as FGFR3 inhibitors using purine as a central scaffold. The two substituents, a polyhydroxylated ribose mimic and a lipophilic moiety, were linked either in position 2 or 6 of the purine ring in order to explore any possible binding mode. All the compounds were able to inhibit FGFR3 kinase activity ...

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