Abstract
Background/Aim: In the search for new derivatives of anthracycline antibiotics, formamidinodaunorubicins containing in the amidine group either a morpholine moiety (DAUFmor) or a hexamethyleneimine moiety (DAUFhex) were synthesized. The biological effects of daunorubicin (DAU), DAUFmor and DAUFhex were compared. Materials and Methods: The experiments were performed on human acute lymphoblastic leukemia MOLT-4 cells and human acute myeloblastic leukemia ML-1 cells. The research was conducted using the spectrophotometric 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) assay and the electronic Beckman-Coulter method. Results: Temporary changes in the leukemia cell viability, size and count were found. The antileukemic activities of the new DAU analogs were weaker than that of daunorubicin. MOLT-4 cells were more sensitive than ML-1 cells to the action of all agents. Among the formamidinodaunorubicins, DAUFmor appeared to be more active in ML-1 cells than DAUFhex, but there were not differences between the analyzed values in MOLT-4 cells. Conclusion: The structural modifications of daunorubicin were responsible for the different antileukemic potentials of the two formamidinodaunorubicins.
- Daunorubicin derivatives
- human acute leukemia cells
- cell viability
- cell volume and count
- in vitro antileukemic activity
- Received August 30, 2012.
- Revision received October 14, 2012.
- Accepted October 15, 2012.
- Copyright© 2012 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved