Investigating the Activity of Indole-2-on Derivative Src Kinase Inhibitors Against Chronic Myeloid Leukemia Cells

Author:

Olgen Sureyya1ORCID,Cort-Donmez Aysegul2ORCID,Guner Ersin3ORCID,Akgun-Cagliyan Gulsum4ORCID,Hanikoglu Ferhat5,Tunc-Ata Melek6,Kilic-Toprak Emine6

Affiliation:

1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University 34010, İstanbul, Turkey

2. Department of Medical Biochemistry, Faculty of Medicine, Pamukkale University 20160, Denizli, Turkey

3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University 34010, İstanbul, Turkey

4. Department of Hematology, Faculty of Medicine, Pamukkale University, Denizli, Turkey

5. Department of Medical Biochemistry, Alanya Alaaddin Keykubat University 07450, Alanya, Antalya, Turkey

6. Department of Physiology, Faculty of Medicine, Pamukkale University, Denizli, Turkey

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.

Funder

Pamukkale University Scientific Research Projects

TUBITAK Scientific Research Funds

Publisher

Bentham Science Publishers Ltd.

Subject

Cancer Research,Pharmacology,Molecular Medicine

Cited by 1 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

1. Preface;Anti-Cancer Agents in Medicinal Chemistry;2024-01

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