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. 2017 Feb 15;27(4):862-866.
doi: 10.1016/j.bmcl.2017.01.015. Epub 2017 Jan 9.

Discovering novel 7-azaindole-based series as potent AXL kinase inhibitors

Clémence Feneyrolles  1 , Léa Guiet  1 , Mathilde Singer  1 , Nathalie Van Hijfte  1 , Bénédicte Daydé-Cazals  1 , Bénédicte Fauvel  1 , Gwénaël Chevé  1 , Abdelaziz Yasri  2
Affiliations

Discovering novel 7-azaindole-based series as potent AXL kinase inhibitors

Clémence Feneyrolles et al. Bioorg Med Chem Lett. .

Abstract

AXL is a receptor tyrosine kinase that plays a key role in tumor growth and proliferation. The scientific community has validated AXL as therapeutic target in the treatment of cancers for several years now, and several AXL inhibitors have been developed but none of them are approved. In this context, we started to design new kinase inhibitors targeting AXL from the 7-azaindole scaffold well known to interact with the ATP binding site of the kinase. Focused screening and chemical diversification around 7-azaindole scaffold were developed, based on modeling studies and medicinal chemistry rational, leading to the discovery of a new family of hits with potent inhibitory activity against AXL.

Keywords: 7-Azaindole; AXL; Kinase inhibitor; Medicinal chemistry; Modeling study; Receptor tyrosine kinase.

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