Table of Contents
Metal-Based Drugs
Volume 3, Issue 2, Pages 101-112

Cytotoxicity and Antineoplastic Activities of Alkylamines and Their Borane Derivatives

1Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360, NC, USA
2Pharmacy B.S. Honors Student, USA
3Summer Research Apprenticeship for Minority Students Program, Mathematics and Science Education Network Pre-College Program, CB#3500, 309 Peabody Hall, –Babes-Bolyai– University, Chapel Hill 27599-3500, NC, USA

Received 12 February 1996; Accepted 5 March 1996

Copyright © 1996 Hindawi Publishing Corporation. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


The alkylamines and their related boron derivatives demonstrated potent cytotoxicity against the growth of murine and human tissue cultured cells. These agents did not necessarily require the boron atom to possess potent cytotoxic action in certain tumor lines. Their ability to suppress tumor cell growth was based on their inhibition of DNA and protein syntheses. DNA synthesis was reduced because purine synthesis was blocked at the enzyme site of IMP dehydrogenase by the agents. In addition ribonucleotide reductase and nucleoside kinase activities were reduced by the agents which would account for the reduced d[NTP] pools. The DNA template or molecule may be a target of the drugs with regard to binding of the drug to nucleoside bases or intercalaction of the drug between DNA base pairs. Only some Of the agents caused DNA fragmentation with reduced DNA viscosity. These effects would contribute to overall cell death afforded by the agents.