Abstract
This report identifies a group of compounds, polymethylene bisacetamides (acetylated diamines), which are potent inducers of erythroid differentiation in murine erythroleukemia cells. A known inducing agent, N-methylacetamide, was dimerized through varying numbers of methylenes in an attempt to increase the local effective concentration at adjacent target sites. The simple dimer was no more effective than N-methylacetamide alone; introduction of five to eight methylenes between acetamide groups substantially increased the effectiveness of these compounds. The hexamethylene bisacetamide was active between 0.5 mM and 5 mM; the percentage of cells induced and the rate at which they were recruited to differentiation was dependent upon the concentration of inducer within this range. At 5 mM hexamethylene bisacetamide essentially the entire population (greater than 99%) was induced to a pathway of erythroid differentiation which was greater differentiation of the cultured cells than with any inducer yet tested.
MeSH Terms
Acetamides/pharmacology
Benzidines/metabolism
Cell Differentiation/drug effects
Cell Line
Dimethyl Sulfoxide/pharmacology
Hemoglobins/biosynthesis
Leukemia, Erythroblastic, Acute/metabolism,pathology
Structure-Activity Relationship
Chemicals
Acetamides
Benzidines
Hemoglobins
Dimethyl Sulfoxide
Authors & Affiliations
5 authors, click to expand affiliations / ORCID
Reuben R C
Wife R L
Breslow R
Rifkind R A
Marks P A
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