[1] First derived from the thermophilic actinomycete Streptomyces refuineus by M. D. Tendler and S Korman in the 1950s, it was first successfully synthesized in a laboratory setting by Leimgruber et al. in 1965.

The chemical structure of anthramycin was first elucidated by Leimgruber using nuclear magnetic resonance and ultraviolet spectroscopy.

The structure of the species was narrowed down to one of two possible candidates: one with a pyrrolobenzodiazepine nucleus, and another with a pyridoquinazoline skeleton.

Acute tissue necrosis has also been noted at the injection site of the antibiotic, and side effect of its high cytotoxicity.

Alternatives such as doxorubicin are today more widely available and prescribed, due to more mild side effects along with increased anti-tumor action.