1986 Volume 50 Issue 7 Pages 1757-1764
β-, γ-, δ- and aza-β-lactam, and thiaziadine compounds induced the differentiation of Friend leukemia cells and hemoglobin was produced. Modification of the lactam rings of γ- and δ-lactam compounds with aromatic side chains and bromine atoms enhanced their differentiation-inducing-activities to Friend leukemia cells. On the other hand, 4 thiaziadine compounds (AKT-1, AKT-2, AKT-3 and AKT-4), which commonly contain a -N(CH3)-N(CH3)-moiety, also promoted the differentiation of Friend leukemia cells. They had specific differentiation-inducing-abilities without toxic effects to Friend leukemia cells. 5-Aza-β-lactam compounds showed differentiation-inducing-activity toward all of three types of Friend leukemia cells, two of which were dimethylsulfoxide (DMSO)-sensitive and the other of which was DMSO-resistant. But we did not find any correlation between the differentiation-inducing-activity and the chemical group at the 1-imino position. The presence of an amino bond, which commonly exist in differentiation agents, was suggested to be necessary for the induction of the differentiation of Friend leukemia cells, and this ability was enhanced with the addition of aromatic side groups.
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