Antineoplastic Agents. 36. Acetylenic Carrier Groups

George Pettit, Edris I. Saldana

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


The development of experimentally facile routes to N-(2-chloroethyl)amines with multifunctional carrier groups was an initial objective of our efforts to design site specific2 (e.g., central nervous system) cancer chemotherapeutic agents. Methods were eventually uncovered for utilizing N-bis(2-chloroethyl)amine in Mannich reactions with, for example, ketones and imides (for leading references see ref 3 and 4). Of the common active hydrogen type compounds generally employed in Mannich reactions the acetylenic carbinols 1 proved most resistant to reaction with N-bis(2-chloroethyl)amine. However, an appropriate copper-catalyzedt procedure was eventually found and acetylenic Mannich bases 2a-d were prepared.3 Subsequent biological evaluation of these substances under the direction of the National Cancer Institute led to the results shown in Table I.6 Because of the promising inhibition shown by the acetylenic Mannich base 2a against murine P-388 lymphocytic leukemia, the present study was undertaken to explore this structural lead and further scope of the copper-catalyzed reaction with N-bis(2-chloroethyl) amine.

Original languageEnglish (US)
Pages (from-to)896-898
Number of pages3
JournalJournal of Medicinal Chemistry
Issue number8
StatePublished - Aug 1 1974

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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