2-[(Arylmethyl)amino]-2-methyl-1,3-propanediol DNA intercalators. An examination of the effects of aromatic ring variation on antitumor activity and DNA binding

• Published in: Journal of medicinal chemistry Vol. 34; no. 7; pp. 1983 - 1990
• Main Authors: Bair, Kenneth W, Andrews, C. Webster, Tuttle, Richard L, Knick, Vincent C, Cory, Michael, McKee, David D
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 01.07.1991
• Subjects: Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - therapeutic use; Chemical Phenomena; Chemistry; Chrysenes - chemical synthesis; Chrysenes - therapeutic use; DNA - metabolism; Intercalating Agents - chemical synthesis; Intercalating Agents - therapeutic use; Leukemia P388 - drug therapy; Mice; Propylene Glycols - chemical synthesis; Propylene Glycols - therapeutic use; Structure-Activity Relationship

The effects of variation of aromatic ring size, shape, and side-chain position on antitumor activity and DNA binding in a series of carbocyclic 2-[(arylmethyl)amino]-2-methyl-1,3-propanediols (AMAPs) were examined. In general, the interaction of AMAPs with DNA increases as the intercalating ring sys...