Design and Synthesis of New Sulfonamides-Based Flt3 Inhibitors.
Med Chem
; 16(3): 403-412, 2020.
Article
in En
| MEDLINE
| ID: mdl-30931863
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.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Sulfonamides
/
Protein Kinase Inhibitors
/
Fms-Like Tyrosine Kinase 3
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Med Chem
Journal subject:
QUIMICA
Year:
2020
Document type:
Article
Affiliation country:
Jordan
Country of publication:
HOLANDA
/
HOLLAND
/
NETHERLANDS
/
NL
/
PAISES BAJOS
/
THE NETHERLANDS