Synthesis and Evaluation of New Derivatives of Busulfan as an Anti-carcinogenic Drug against k562 Cancer Cells Using the AO / PI Method

Hadi Jabbari1, *
, Setareh Khosravi2
, Saeid Azimi1

1 Department of Chemistry, Payame Noor University, P.O. Box 19395-3697Tehran, Iran
2 Departmentof Orthodontics, School of Dentistry, Alborz University of Medical Science, Karaj, Iran

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© 2022 Jabbari et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Department of Chemistry, Payame Noor University, P.O. Box 19395-3697 Tehran, Iran; Tel: 989143615355; E-mail:



Busulfan is a DNA alkylating drug used to treat chronic myeloid leukemia (CML). This type of leukemia affects bone marrow cells or myocytes, which make up bone marrow tissue having a chronic process. Leukemia is a progressive and malignant disease of the body's hematopoietic organs. The disease is caused by the underdevelopment and proliferation of white blood cells and their precursors in the blood and bone marrow.


The synthesis of Busulfan drug and the conjugation of Busulfan from the anomeric position of acetylated galactose as a new derivative of Busulfan and its anti-cancer effect on K562 cancer cells are among the most important objectives of this study.


In this work, galactose was acetylated with acetic anhydride in the presence of sodium acetate, then the anomeric position of acetylated carbohydrate deacetylated using imidazole to obtain the final product through the reaction of Busulfan. Anti-cancer activity of the product was evaluated against K562 cancer cells. The proliferation and survival of K562 cancer cells and PBMCs (peripheral blood mononuclear cells) using the AO/PI method were studied. Furthermore, 1- (2, 3, 4, 6-tetra-O-acetyl-Iβ-D-galactopyranosyl) -4- (methyl sulfonyl oxy) butane was evaluated against cancer cells as a new derivative.


In this study, the Acridine Orange / Propidium Iodide (AO/PI) method was performed using fluorescence microscopy to evaluate the efficacy of a synthesized product. The effective dose of 0.02 mg/L of 1- (2, 3, 4, 6-tetra-O-acetyl-Iβ-D-galactopyranosyl) -4- (methyl sulfonyl oxy) butane was observed to cause 96% of cancer cells necrosis.


1- (2, 3, 4, 6-tetra-O-acetyl-Iβ-D-galactopyranosyl) -4- (methyl sulfonyl oxy) butane as a new derivative of Busulfan acts non-specifically in the cell cycle by inhibiting DNA activity by alkylation and binding to the DNA strand. Alkylating agents usually bind an alkyl group to the number seven nitrogen atom in the guanine nucleotide in a DNA molecule.

Keywords: Busulfan, K562 cancer cell, Carbohydrate, Anomeric position, Efficacy evaluation, Chronic myeloid leukemia.