Conformationally constrained inhibitors of caspase-1 (interleukin-1β converting enzyme) and of the human ced-3 homologue caspase-3 (CPP32, apopain)

A systematic study of interleukin-1β converting enzyme (ICE, caspase-1) and caspase-3 (CPP32, apopain) inhibitors incorporating a P2–P3 conformationally constrained dipeptide mimetic is reported. Depending on the nature of the P4 substituent, highly selective inhibitors of both Csp-1 or Csp-3 were obtained.