877060-48-5Relevant academic research and scientific papers
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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Page/Page column 48; 49, (2011/04/25)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di
Rapid preparation of triazolyl substituted NH-heterocyclic kinase inhibitors via one-pot Sonogashira coupling-TMS-deprotection-CuAAC sequence
Merkul, Eugen,Klukas, Fabian,Dorsch, Dieter,Graedler, Ulrich,Greiner, Hartmut E.,Mueller, Thomas J. J.
, p. 5129 - 5136 (2011/09/13)
The one-pot, three-component Sonogashira coupling-TMS-deprotection-CuAAC ("click") sequence is the key reaction for the rapid synthesis of triazolyl substituted N-Boc protected NH-heterocycles, such as indole, indazole, 4-, 5-, 6-, and 7-azaindoles, 4,7-diazaindole, 7-deazapurines, pyrrole, pyrazole, and imidazole. Subsequently, the protective group was readily removed to give the corresponding triazolyl derivatives of these tremendously important NH-heterocycles. All compounds have been tested in a broad panel of kinase assays. Several compounds, 8f, 8h, 8k, and 8l, have been shown to inhibit the kinase PDK1, a target with high oncology relevance, and thus they are promising lead structures for the development of more active derivatives. The X-ray structure analysis of compound 8f in complex with PDK1 has revealed the detailed binding mode of the molecule in the kinase. The Royal Society of Chemistry 2011.
Versatile and convenient methods for the synthesis of C-2 and C-3 functionalised 5-azaindoles
Lefoix, Myriam,Daillant, Jean-Philippe,Routier, Sylvain,Merour, Jean-Yves,Gillaizeau, Isabelle,Coudert, Gerard
, p. 3581 - 3588 (2007/10/03)
Functionalisation at C-2 and C-3 of N-protected-5-azaindole leads to a variety of very useful new substituted 5-azaindole derivatives in fair to good yields. Georg Thieme Verlag Stuttgart.
