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Communication | Special issue | Vol 13, No. 1, 1979, pp.469-476
Published online, 1st January, 1970
DOI: 10.3987/S-1979-01-0469
Pepleomycin, the Second Generation Bleomycin Chemically Derived from Bleomycin A2

Wataru Tanaka* and Tomohisa Takita

*Pharmaceutical Division, Nippon-Kayaku Co. Ltd., 3-31-12, Shimo, Kita, Tokyo 115-0042, Japan

Abstract

Pepleomycin, 3-(S-1-phenylethylamino)-propylaminobleomycin, has been synthesized from bleomycin A2, the main component of natural bleomycins, by a series of the following reactions: demethylation, cyclic iminoether formation, hydration and aminolysis with 3-(S-1-phenylethylamino)-propylamine. Pepleomycin has stronger activity and less pulmonary toxicity than natural bleomycin mixture clinically used today in the treatment of cancer and will become the second generation bleomycin in its cancer therapy.