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Issue 9, 2010
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Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors

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Abstract

A library of pyrido[2,3-d]pyrimidines was designed as inhibitors of FGFR3 tyrosine kinase allowing possible interactions with an unexploited region of the ATP binding-site. This library was built-up with an efficient step of click-chemistry giving easy access to triazole-based compounds bearing a large panel of substituents. Among the 27 analogues synthesized, more than half exhibited 55–89% inhibition of in vitro FGFR3 kinase activity at 2 μM and one (19g) was able to inhibit auto-phosphorylation of mutant FGFR3-K650M in transfected HEK cells.

Graphical abstract: Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors

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Publication details

The article was received on 13 Nov 2009, accepted on 17 Feb 2010 and first published on 11 Mar 2010


Article type: Paper
DOI: 10.1039/B923882D
Org. Biomol. Chem., 2010,8, 2164-2173

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    Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors

    L. Le Corre, A. Girard, J. Aubertin, F. Radvanyi, C. Benoist-Lasselin, A. Jonquoy, E. Mugniery, L. Legeai-Mallet, P. Busca and Y. Le Merrer, Org. Biomol. Chem., 2010, 8, 2164
    DOI: 10.1039/B923882D

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