title: Effects of structural modifications of daunorubicin on in vitro antileukemic activity.
abstract: OBJECTIVE
  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.
  
  
  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.
  
  
  CONCLUSIONS
  The structural modifications of daunorubicin were responsible for the different antileukemic potentials of the two formamidinodaunorubicins.
authors.affiliation: Department of Experimental Hematology, Jagiellonian University, Gronostajowa 9, 30-387 Cracow, Poland.
authors.forename: Marta
authors.initials: M
authors.lastname: Stojak
authors.forename: Lidia
authors.initials: L
authors.lastname: Mazur
authors.forename: Malgorzata
authors.initials: M
authors.lastname: Opydo-Chanek
authors.forename: Malgorzata
authors.initials: M
authors.lastname: Lukawska
authors.forename: Irena
authors.initials: I
authors.lastname: Oszczapowicz
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D003630:Daunorubicin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D054198:Precursor Cell Lymphoblastic Leukemia-Lymphoma / Q000188:drug therapy*; D013329:Structure-Activity Relationship
chemical_list: D000903:Antibiotics, Antineoplastic; D003630:Daunorubicin