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

Clémence Feneyrolles1, Léa Guiet1, Mathilde Singer1

  • 1OriBase Pharma, Cap Gamma, Parc Euromédecine, 1682 rue de la Valsière, CS 17383, 34189 Montpellier Cedex 4, France.

Bioorganic & Medicinal Chemistry Letters
|January 18, 2017
PubMed

Insights

Researchers designed novel 7-azaindole-based inhibitors targeting the receptor tyrosine kinase AXL, a key driver in cancer proliferation. This work identified a new class of potent AXL inhibitors for potential cancer therapies.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Biochemistry

Background:

  • AXL receptor tyrosine kinase is a validated therapeutic target in oncology due to its role in tumor growth and proliferation.
  • Despite years of research and development, no AXL inhibitors have received regulatory approval for cancer treatment.

Purpose of the Study:

  • To design and discover novel kinase inhibitors targeting AXL using a 7-azaindole scaffold.
  • To identify potent AXL inhibitors with potential therapeutic applications in cancer treatment.

Main Methods:

  • Utilized a 7-azaindole scaffold, known to interact with the ATP binding site of kinases.
  • Employed focused screening and chemical diversification strategies.
  • Incorporated computational modeling and medicinal chemistry principles.

Main Results:

  • Discovered a new family of chemical compounds exhibiting potent inhibitory activity against AXL.
  • Identified promising hits through structure-based design and screening.

Conclusions:

  • The 7-azaindole scaffold is a viable starting point for developing novel AXL inhibitors.
  • The identified compounds represent a promising new class of potential therapeutics for AXL-driven cancers.
Keywords:
7-AzaindoleAXLKinase inhibitorMedicinal chemistryModeling studyReceptor tyrosine kinase

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