The design and synthesis of new pyrido[3,4-g]quinazoline derivatives is described as well as their protein kinase inhibitory potencies toward five CMGC family members (CDK5, CK1, GSK3, CLK1 and DYRK1A). The interest for this original tricyclic heteroaromatic scaffold as modulators of CLK1/DYRK1A activity was validated by nanomolar potencies (compounds 12 and 13). CLK1 co-crystal structures with two inhibitors revealed the binding mode of these compounds within the ATP-binding pocket.
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| http://dx.doi.org/10.1016/j.ejmech.2016.04.004 | DOI Listing |
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Catalyst and solvent switched divergent C-H functionalization: oxidative annulation of N-aryl substituted quinazolin-4-amine with alkynes.
Org Biomol Chem
April 2020
Department of Chemistry, Osmania University, Hyderabad-500 007, India.
The development of site-selective C-H functionalizations/annulations is one of the most challenging practices in synthetic organic chemistry particularly for substrates bearing several similarly reactive C-H bonds. Herein, we describe catalyst and solvent controlled ortho/peri site-selective oxidative annulation of C-H bonds of N-aryl substituted quinazolin-4-amines with internal alkynes. The ortho C-H selective annulation was observed using Pd-catalyst in DMF to give indole-quinazoline derivatives, while, Ru-catalyst in PEG-400 favoured the peri C-H bond annulation exclusively to furnish pyrido-quinazoline derivatives.
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