Structure activity relationship of antiproliferative N-acyl-beta-alanine amides.
Starting from the antiproliferative N-homofarnesoyl-beta-alanine amide 1 as a lead structure we have demonstrated that the homofarnesoyl residue of 1 can be replaced by several aliphatic and aromatic acyl moieties which offer advantages in terms of availability and stability over the original homofarnesoyl residue. The N-(2,3-dimethylphenyl) aminosulfonylphenyl moiety of 1 turned out to be essential for antiproliferative activity and cannot be replaced without complete loss of activity.
Schlitzer
M
M
Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, D-35032 Marburg. schlitze@mailer.uni-marburg.de
Dahse
H M
HM
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D005204:Farnesol / Q000031:analogs & derivatives* / Q000737:chemistry; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D005204:Farnesol