7556-93-6Relevant articles and documents
Insights into the modular design of kinase inhibitors and application to Abl and Axl
Johnson, Taylor K.,Lachacz, Eric J.,Lopez-Barcons, Lluis,Merajver, Sofia D.,Phadke, Sameer,Soellner, Matthew B.,Vandecan, Nathalie,Wu, Zhifen
, p. 64 - 71 (2022/02/26)
Scaffold hopping is a common strategy for generating kinase inhibitors that bind to the DFG-out inactive conformation. Small structural differences in inhibitor scaffolds can have significant effects on potency and selectivity across the kinome, however, these effects are often not studied in detail. Herein, we outline a design strategy to generate an array of DFG-out conformation inhibitors with three different hinge-binders and two DFG-pocket groups. We studied inhibitor selectivity across a large segment of the kinome and elucidated binding preferences that can be used in scaffold hopping campaigns. Using these analyses, we identified two selective inhibitors that display low nanomolar potency against Axl or wild-type and clinically relevant mutants of Abl.
Synthesis and anti-oomycete activity of novel quinazolin- and benzothiazol-6-yloxyacetamides: Potent aza-analogs and five-ring analogs of quinoline fungicides
Beaudegnies, Renaud,Quaranta, Laura,Murphy Kessabi, Fiona,Lamberth, Clemens,Knauf-Beiter, Gertrud,Fraser, Torquil
, p. 444 - 452 (2016/01/25)
Novel quinazolin- and benzothiazol-6-yloxyacetamides show excellent in vivo activity against the three economically most important Oomycete pathogens Phytophthora infestans, Plasmopara viticola and Pythium ultimum. They are polar analogs of known quinolin-6-yloxyacetamides, which are not active against the soil-borne damping-off disease caused by Pythium ultimum. The Bogert quinazoline synthesis, an almost forgotten heterocyclization technique, proved to be highly useful for the concise construction of required quinazolin-6-ol building blocks.
An original method for the synthesis of quinazolines
Aksenov,Lyakhovnenko,Kugutov
body text, p. 125 - 126 (2010/08/05)
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