Skip to content
2000
Volume 16, Issue 3
  • ISSN: 1573-4064
  • E-ISSN: 1875-6638

Abstract

Background: Flt3 is an oncogenic kinase involved in different leukemias. It is most prominently associated with acute myeloid leukemia (AML). Flt3-specific inhibitors have shown promising results in interfering with AML. Methods: The crystallographic structures of two inhibitors complexed within Flt3, namely, quizartinib and F6M, were used to guide the synthesis of new sulfonamide-based Flt3 inhibitors. Results: One of the prepared compounds showed low micromolar anti-Flt3 bioactivity, and interestingly, low micromolar bioactivity against the related oncogenic kinase VEGFR2. Conclusion: Sulfonamides were successfully used as privileged scaffolds for the synthesis of novel Flt3 inhibitors of micromolar potencies.

Loading

Article metrics loading...

/content/journals/mc/10.2174/1573406415666190401144053
2020-05-01
2025-06-20
Loading full text...

Full text loading...

/content/journals/mc/10.2174/1573406415666190401144053
Loading

  • Article Type:
    Research Article
Keyword(s): Acute Myeloid Leukemia; F6M; Flt3; Quizatrinib; Sulfonamides; VEGFR2
This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error
Please enter a valid_number test