First synthesis and pharmacological evaluation of benzoindolizidine and benzoquinolizidine analogues of alpha- and beta-peltatin.

The benzoindolizidine and quinolizidine analogues of alpha- and beta-peltatin were designed and synthesized by two different synthetic routes involving as the key step the Bischler-Napieralski cyclization of suitably substituted N-acyl-2-arylmethylpyrrolidine and -piperidine derivatives. The in vitro biological activity of these analogues as well as some of their derivatives was subsequently evaluated.