Chlamydocin is a powerful in vitro antitumoral agent, quickly inactiva
ted in vivo. A series of cyclic tetrapeptides related to chlamydocin o
r HC toxin and bearing a bioactive alkylating group on an epsilon-amin
o-lysyl function have been examined for their antitumoral activity on
L1210 and P388 murine leukemia cell lines. One analog was found to be
potent at inhibiting L1210 cell proliferation and had a higher therape
utic index than the reference compound bis-beta-chloroethylnitrosourea
on the in vivo P388-induced leukemia model.