Antitumor activity and some pharmacologic properties of anthramycin methyl ether.

The antitumor antibiotic, anthramycin methyl ether (AME), was shown to be active in increasing survival time in mice bearing various experimental leukemias. Like actinomycin D, it was active against P388 but inactive against P388/38280. AME also was active against the plasma cell tumor LCP, while having no activity against the plasma cell tumor YPC-1. AME bad an IDso of 0.02/~g/ml against L1210 cells in tissue culture. The effects of AME were studied on other pharmacologic parameters. Hexobarbital sleeping times were doubled in mice receiving daily injections of AME for 4 days, while single injections at times varying from 30 minutes to 4 hours prior to hovoharl~ital harl nr~ effect on sleeping time. A ~,.rw 'lid not ",~,,~+ the blood pressure, respiration, or EKG in anesthetized dogs, nor did it alter the blood pressure responses to various autonomic stimulants. AME markedly inhibited uptake of tritiated uridine in both L1210 and P3S8 leukemic cells in vivo. AME also interfered with uptake of tritiated thymidine by L12t0 cel}s. Spectra1 studies indicated that the uItraviolet absorption maximum of AME was shifted to longer wave lengths following interaction