Evolution of cancer chemotherapy

Louis S. GoodmanLouis S. Goodman
Alfred GilmanAlfred Gilman

Evolution of cancer chemotherapy

The use of chemicals to treat cancer (cancer chemotherapy) started in 1942 with the clinical use of nitrogen mustards by Louis S. Goodman and Alfred Gilman. Subsequent discoveries included mechlorethamine (Mustargen), chlorambucil (1952), and cyclophosphamide (1956). Drugs to block folic acid (also called antimetabolites) were also developed.

How tumours grow

Cancer cell division or proliferation leads to the growth of tumours.


George HitchingsGeorge Hitchings
Charles HeidelbergerCharles Heidelberger

Aminopterin (1947) was effective against leukemia, but its adverse effects on white blood cells quickly led to its replacement by methotrexate. In the 1950s, George Hitchings and Charles Heidelberger developed the antimetabolitic mercaptopurine for leukemia and fluorouracil for gastrointestinal and breast tumours.

Did you know?

It was noted by the U.S. Army's medical workers that the white-cell counts of soldiers exposed to mustard gas —in fact, a toxic liquid—were reduced. Studies on the use of similar chemicals as agents for the treatment of cancers led to the discovery of mustine, and the birth of anticancer chemotherapy.

Mercaptopurine molecule

Fluorouracil molecule