Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Polyamine analogues with antitumor activity.

M L Edwards1, N J Prakash, D M Stemerick

  • 1Merrell Dow Research Institute, Cincinnati, Ohio 45215.

Journal of Medicinal Chemistry
|May 1, 1990
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

First-in-human phase I study of the DNA-repair inhibitor DT01 in combination with radiotherapy in patients with skin metastases from melanoma.

British journal of cancer·2016
Same author

Recombinant factor VIII Fc fusion protein: extended-interval dosing maintains low bleeding rates and correlates with von Willebrand factor levels.

Journal of thrombosis and haemostasis : JTH·2014
Same author

Tissue-and metal-specific effects of thiolacrylic acids in rats.

Biological trace element research·2013
Same author

Biochemical and functional characterization of a recombinant monomeric factor VIII-Fc fusion protein.

Journal of thrombosis and haemostasis : JTH·2012
Same author

[Is proton beam therapy the future of radiotherapy? Part I: clinical aspects].

Cancer radiotherapie : journal de la Societe francaise de radiotherapie oncologique·2010
Same author

Amoebic pericarditis.

The Medical journal of Australia·2010
Same journal

Rational Development of Activatable Prodrugs of the GSTP1 Inhibitor NBDHEX: Turn-On NIR Fluorogenic Drug Delivery with Selective Anticancer Activity.

Journal of medicinal chemistry·2026
Same journal

Recent Highlights in the Discovery and Design of Antibody-Drug Conjugates.

Journal of medicinal chemistry·2026
Same journal

One Face, Three Solutions: Structural Convergence in PD-L1 Inhibition across Antibodies, Macrocycles, and Small Molecules.

Journal of medicinal chemistry·2026
Same journal

A Potent and Selective Quinolone-Based PTPN22 Inhibitor with Improved Immunotherapeutic Activity.

Journal of medicinal chemistry·2026
Same journal

Structure-Based Discovery of (<i>E</i>)- and (<i>Z</i>)-4-Oxobut-2-enoate Derivatives as Novel Covalent Pin1 Inhibitors with Antitumor Activity.

Journal of medicinal chemistry·2026
Same journal

Hybrids of Benzenesulfonamide Oxadiazole Derivatives with Dual CA II and COX-2 Inhibitory Activity Demonstrating Antiglaucoma and Anti-inflammatory Action: Synthesis, In Silico Insights, and In Vitro and In Vivo Bioevaluation.

Journal of medicinal chemistry·2026
See all related articles

New tetraamines derived from 1,8-diaminooctane show promising antitumor activity against mouse leukemia. Combining these agents with a polyamine oxidase inhibitor further enhanced their effectiveness in preclinical models.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Research

Background:

  • The development of novel antitumor agents is crucial for effective cancer therapy.
  • Polyamines play a significant role in cell proliferation and cancer progression.
  • Targeting polyamine metabolism or synthesis presents a viable strategy for cancer treatment.

Purpose of the Study:

  • To synthesize and evaluate a series of novel tetraamines derived from 1,8-diaminooctane as potential antitumor agents.
  • To assess the efficacy of these tetraamines in a preclinical mouse leukemia model.
  • To investigate the synergistic effect of combining these tetraamines with a polyamine oxidase inhibitor.

Main Methods:

  • Synthesis of N,N'-bis(cyanoethyl)-1,8-diaminooctane from 1,8-diaminooctane and acrylonitrile.

Related Experiment Videos

  • Reduction of the dinitrile to a tetraamine (compound 20).
  • Preparation of bis(alkyl)polyamines (compounds 26a and 26b) via alkylation and deprotection of the tetra-Boc derivative.
  • Antitumor activity testing using the mouse L1210 leukemia model.
  • Evaluation of coadministration with a polyamine oxidase inhibitor.

    • Main Results:

    • Three synthesized tetraamine derivatives demonstrated promising antitumor activity in the L1210 leukemia model.
    • The bis(alkyl)polyamines 26a and 26b showed significant efficacy.
    • Coadministration with a polyamine oxidase inhibitor potentiated the observed antitumor effects, indicating a synergistic interaction.

    Conclusions:

    • The novel tetraamines derived from 1,8-diaminooctane represent a promising class of compounds for cancer chemotherapy.
    • The observed potentiation by polyamine oxidase inhibitors suggests a therapeutic strategy involving modulation of polyamine metabolism.
    • Further investigation into the mechanism of action and optimization of these compounds is warranted for clinical development.