Table of Contents
Metal-Based Drugs
Volume 3 (1996), Issue 3, Pages 155-160

Boronated Pyrimidines and Purines as Cytotoxic, Hypolipidemic and Anti-Inflammatory Agents

1Division of Medicinal Chemistry and Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599-7360, North Carolina, USA
2Boron Biologicals, Inc., 620 Hutton Street, Raleigh 27606-1490, North Carolina, USA

Received 19 April 1996; Accepted 1 May 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 simple boronated bases, e.g. cytosine, adenine and guanine, containing no sugar residues retained good pharmacological activity as hypolipidemic, anti-neoplastic and anti-inflammatory agents in mice at 8 mg/kg. Their activities were generally identical to their respective nucleoside derivatives. Interestingly the boronated acyclovir derivative was a very potent hypolipidemic agent achieving better activity than clofibrate and lovastatin. The boronated adenine derivatives appeared to have the best anti-inflammatory activity in reducing local edema and analgesic effects. The agents were active against the growth of murine and human leukemias and human HeLa-S3 suspended uterine carcinoma. Only the boronated adenine derivatives were effective in blocking the growth of human SW480 adenocarcinoma and the KB nasopharynx.