Anti-cancer agents in medicinal chemistry · 2016
In Vitro Anticancer Effects of Two New Potent Hydrazide Compounds on Leukemic Cells.
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Tavakolfar Shahrzad, Mousavi Elham, Almasirad Ali, Amanzadeh Amir, Atyabi Seyyed Mohamamd, Yaghamii Parichehr, Samiee-Sadr Somayeh, Salimi Mona
Аннотация
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.
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.