Differential effects of benzamidine derivatives on the expression of c-myc and HLA-DR alpha genes in a human B-lymphoid tumor cell line.
In this paper, we report the effects of aromatic tetra amidines (TAPP-H) on cell growth and gene expression of a B-lymphoid human tumor cell line, WI-L2. The results obtained give evidence (a) for inhibition of cell proliferation by TAPP-H; (b) for stronger antiproliferative activity of TAPP-halo derivatives; (c) for TAPP-mediated inhibition of accumulation of c-myc RNA sequences but not of HLA-DR alpha mRNA and DR antigens. These results suggest that this class of antiproliferative compounds exhibit differential effects on cell-cycle specific and differentiation specific genes. In addition, also TAPP-related compounds containing 2 (DAPP) or 3 (TAPB) benzamidine residues retain inhibitory activity on the proliferation of WI-L2 cells. These latter compounds might be proposed as useful substrate in the synthesis of drug-conjugated monoclonal antibodies or growth factors.
D000578:Amidines / Q000494:pharmacology*; D001550:Benzamidines / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D005786:Gene Expression Regulation / Q000187:drug effects; D006681:HLA-D Antigens / Q000235:genetics*; D006684:HLA-DR Antigens / Q000032:analysis / Q000235:genetics*; D006801:Humans; D011480:Protease Inhibitors / Q000494:pharmacology*; D011519:Proto-Oncogenes; D012313:RNA / Q000032:analysis; D014407:Tumor Cells, Cultured / Q000187:drug effects*
D000578:Amidines; D001550:Benzamidines; D006681:HLA-D Antigens; D006684:HLA-DR Antigens; D011480:Protease Inhibitors; D012313:RNA; C032157:benzamidine