Investigating the Activity of Indole-2-on Derivative Src Kinase Inhibitors Against Chronic Myeloid Leukemia Cells.
Anticancer Agents Med Chem
; 23(1): 113-122, 2023.
Article
en En
| MEDLINE
| ID: mdl-35570519
ABSTRACT
BACKGROUND:
Src family tyrosine kinases play a potential role in Bcr-Abl-induced leukemogenesis. Src kinase inhibitors are reported as selective inhibitors of chronic myeloid leukemia.OBJECTIVE:
Since Src kinase inhibitors have an inhibitive effect on chronic myeloid leukemia, indole derivatives (C-1, C-2, C-3) previously found as potent inhibitors of Src kinase were tested against chronic myeloid leukemia in this study.METHODS:
Cell viability of K562 and R/K562 cells, antiproliferative and antioxidant effects, and inhibition profiles of Bcr-Abl kinase of indole derivatives were determined compared to dasatinib and imatinib.RESULTS:
The results showed that compounds affected cell proliferation and decreased the levels of Bcr/Abl. These results confirmed that the antileukemic activity of compounds was related to Bcr/Abl expression. Docking studies also presented that compounds are inhibitors of both Src and Abl kinases. Calculation of drug-like properties showed that compounds could be potential drug candidates.CONCLUSION:
Among indole-2-on derivatives, previously identified as Src kinase inhibitors, C-2 has been discovered to be a strong anticancer drug that is active against susceptible and resistant K562 cell lines and induces apoptosis.Palabras clave
Texto completo:
1
Colección:
01-internacional
Asunto principal:
Leucemia Mielógena Crónica BCR-ABL Positiva
/
Familia-src Quinasas
/
Inhibidores de Proteínas Quinasas
Límite:
Humans
Idioma:
En
Revista:
Anticancer Agents Med Chem
Asunto de la revista:
ANTINEOPLASICOS
/
QUIMICA
Año:
2023
Tipo del documento:
Article
País de afiliación:
Turquía