These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Evaluation of Mannich bases of styryl ketones and related hydrazones for activity against P388 leukemia.
    Author: Dimmock JR, Jonnalagadda SS, Leek DM, Warrington RC, Fang WD.
    Journal: Neoplasma; 1988; 35(6):715-24. PubMed ID: 3221938.
    Abstract:
    A Mannich base namely 4-dimethylaminomethyl-1-phenyl-1-penten-3-one hydrochloride was shown to have far greater activity than 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) towards P388 leukemia cells in vitro. However, the compound was inactive in an in vivo P388 murine screen, and the object of this study was to discern molecular features which conferred in vivo activity. Mannich bases containing electron-attracting substituents in the aryl ring had in vivo potency in contrast to the analogs which had electron-donating groups in the ring. A number of hydrazones of the Mannich bases were prepared as potential prodrugs and did not enhance bioactivity. This observation was probably due to a lack of facile hydrolysis of the hydrazones to the corresponding Mannich bases in vivo since high resolution 1H NMR spectroscopy revealed that representative hydrazones either did not regenerate the ketones or produced them only in minute quantities at pH values normally encountered in living tissues.
    [Abstract] [Full Text] [Related] [New Search]