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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Research Article

In Vitro Anticancer Effects of Two New Potent Hydrazide Compounds on Leukemic Cells

Author(s): Shahrzad Tavakolfar, Elham Mousavi, Ali Almasirad, Amir Amanzadeh, Seyyed Mohamamd Atyabi, Parichehr Yaghamii, Somayeh Samiee-Sadr and Mona Salimi

Volume 16, Issue 12, 2016

Page: [1646 - 1651] Pages: 6

DOI: 10.2174/1871520616666160404112945

Price: $65

Abstract

Background: Chronic myeloid leukemia (CML), also recognized as chronic myelogenous leukemia, is initiated in some types of blood-forming cells of the bone marrow. The therapeutic approach to CML is usually chemotherapy; however, severe side effects and complications are major problems in the clinical research. Thus, recent efforts have focused on the search for compounds affecting apoptosis in this type of cancer.

Objective: In this study, in vitro anticancer activity of two compounds (A and B) consisting of a hydrazide backbone with nitro-thiophen and furan substituents was assessed against K562 cell line displaying certain levels of sensitivity to pro-apoptotic compounds.

Methods: The anticancer activity was assessed using MTT assay, flowcytometry, annexin-V and Western blot analysis.

Results: Compounds A and B were both active and revealed a remarkable in vitro cytotoxic effect showing IC50 values of 0.09 and 0.07 μM, respectively, after 72 h of treatment. A significant increase in annexin-V/PI staining, sub-G1 population and Bax/Bcl-2 ratio revealed the apoptotic cell death of compounds A- and B-treated K562 cells.

Conclusion: The results presented here could be used as a first step for the development of powerful chemotherapeutic agents to treat leukemia.

Keywords: Leukemia, apoptosis, cancer, hydrazide.

Graphical Abstract

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