Differential effects of benzamidine derivatives on the expression of c-myc and HLA-DRα 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 experession 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-DRα mRNA and DR antigens. These results suggest that this class of antiproliferative compounds exibit 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. © 1988.