SYNTHESIS AND ANTIPROLIFERATIVE ACTIVITY OF SPIROCYCLIC CYCLODIPEPTIDES, DERIVATIVES OF 1-AMINO-1-CYCLOBUTANECARBOXYLIC ACID

A series of chiral spirocyclic cyclodipeptides of the general formula I was synthesized; the aim was to determine how the substitution of cy clobutane for cyclopentane in cyclo(-alanyl-1-amino-1-cyclopentanecarb onyl-) would influence the inhibition of the proliferative activity of the caudal morphogenetic system (CMS) of chick embryos. Spirocyclic c yclodipeptides Ia - Il were obtained by cyclization of linear dipeptid es IIa - IIf, prepared by condensation of protected amino acids by DCC I method. The inhibition was investigated by the Chick Embryotoxicity Screening Test. The results show generally lower activity in the teste d series, as compared with derivatives containing 1-amino-1-cyclopenta necarboxylic acid.