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State-of-the-art of small molecule inhibitors of the TAM family: the point of view of the chemist.
The TAM family of tyrosine kinases receptors (Tyro3, Axl and Mer) is implicated in cancer development, autoimmune reactions and viral infection and is therefore emerging as an effective andExpand
Design, synthesis, biological evaluation and cellular imaging of imidazo[4,5-b]pyridine derivatives as potent and selective TAM inhibitors.
The TAM kinase family arises as a new effective and attractive therapeutic target for cancer therapy, autoimmune and viral diseases. A series of 2,6-disubstituted imidazo[4,5-b]pyridines wereExpand
Direct Alkynylation of 3H-Imidazo[4,5-b]pyridines Using gem-Dibromoalkenes as Alkynes Source.
C2 direct alkynylation of 3H-imidazo[4,5-b]pyridine derivatives is explored for the first time. Stable and readily available 1,1-dibromo-1-alkenes, electrophilic alkyne precursors, are used asExpand
Microwave-Assisted C-2 Direct Alk­enylation of Imidazo[4,5-b]pyr­idines: Access to Fluorescent Purine Isosteres with Remarkably Large Stokes Shifts
We describe herein the first C-2 direct alkenylation of the valuable 3H-imidazo[4,5-b]pyridine promoted by microwave-assisted Pd/Cu co-catalysis. The reaction is rapid and compatible with a wideExpand
Stealth fluorescence labeling for live microscopy imaging of mRNA delivery
Methods for tracking of RNA molecules inside living cells are critical to probe their dynamics and biological functions, but also to monitor delivery of therapeutic RNA. We here describe a method forExpand
Sulfonylguanidine Derivatives as Potential Antimelanoma Agents
Sulfonylguanidines are interesting bioactive compounds with a broad range of applications in the treatment of different pathologies. 2‐Aminobenzazole‐based structures are well employed in theExpand
Fluorescent base analogues in gapmers enable stealth labeling of antisense oligonucleotide therapeutics
To expand the antisense oligonucleotide (ASO) fluorescence labeling toolbox beyond covalent conjugation of external dyes (e.g. ATTO-, Alexa Fluor-, or cyanine dyes), we herein explore fluorescentExpand
Stealth Fluorescence Labeling for Live Microscopy Imaging of mRNA Delivery
Methods for tracking RNA inside living cells without perturbing their natural interactions and functions are critical within biology and, in particular, to facilitate studies of therapeutic RNAExpand