Antineoplastic agents LXIV: 1,4‐bis(2′‐chloroethyl)‐1,4‐diazabicyclo[2.2.1]heptane dihydrogen dimaleate

George Pettit, D. P. Gieschen, W. E. Pettit

Research output: Contribution to journalArticlepeer-review

8 Scopus citations


The 1,4‐bis(2′‐chloroethyl)‐1,4‐diazabicyclo[2.2.1]heptane dication (II) exhibits remarkable antineoplastic activity. Detailed evaluation of several dianion derivatives showed a curative response level against the murine P‐388 lymphocytic leukemia, colon 26, CD8F1 mammary, and the Walker 256 carcinosarcoma (rat) tumor systems. In addition, significant cancer chemotherapeutic activity was found against the murine L‐1210 lymphoid leukemia, colon 38, and B16 melanocarcinoma tumor systems. The bicyclo dication (II) first was isolated, evaluated, and stored as the diperchlorate derivative (Ila). Because of the promising anticancer activity of Ila, procedures were developed for obtaining other anion derivatives for comparative biological purposes. Several naturally occurring substances were evaluated, and the dihydrogen dimaleate derivative (IIi) obtained by an ion‐exchange technique was the most suitable.

Original languageEnglish (US)
Pages (from-to)1539-1542
Number of pages4
JournalJournal of Pharmaceutical Sciences
Issue number12
StatePublished - Dec 1979


  • 1,4‐Bis(2′‐chloroethyl)‐1,4‐diazabicyclo‐[2.2.1]heptane cation—antineoplastic activity, synthesis, diperchlorate and dihydrogen dimaleate salts
  • Antineoplastic agents—1,4‐bis(2′ ‐ chloroethyl) ‐ 1,4‐diazabicyclo[2.2.1]heptane cation, synthesis, diperchlorate and dihydrogen dimaleate salts
  • Heterocyclic anticancer agents— 1,4‐bis(2′‐chloroethyl)‐1,4‐diazabicyclo[2.2.1]heptane cation, synthesis, diperchlorate and dihydrogen dimaleate salts

ASJC Scopus subject areas

  • Pharmaceutical Science


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