NUCLEOSIDE PHOSPHATE ANALOGUES WITH BORONATED PHOSPHATES

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$483,092.00
Award Year:
1993
Program:
SBIR
Phase:
Phase II
Contract:
n/a
Agency Tracking Number:
16296
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
Boron Biologicals, Inc.
533 Pylon Drive P O Box 3348, 9, Raleigh, NC, 27636
Hubzone Owned:
N
Socially and Economically Disadvantaged:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
Spielvogel, Bernard F
Principal Investigator
(919) 832-2044
Business Contact:
1 R43 AI30887-01
() -
Research Institution:
n/a
Abstract
USE OF NUCLEOSIDE PHOSPHATES AS ANTITUMOR AND ANTIVIRAL AGENTS HAS BEEN LIMITED BY THEIR INABILITY TO PENETRATE CELL MEMBRANES AS WELL AS THEIR HIGH SUSCEPTIBILITY TO ENZYMES SUCH AS PHOSPHATASES, NUCLEOTIDASES, ETC. MODIFICATION OF THE PHOSPHATE GROUP (BY REPLACING ONE OF THE NONBRIDGING OXYGENS WITH A BORANE GROUP) MAY PROVIDE BOTH THE MEMBRANE PERMEABILITY TO THESE COMPOUNDS AND THE STABILITY (TOWARDS PHOSPHATE-REMOVING ENZYMES). THE LONG- TERM OBJECTIVE OF THIS PROJECT IS TO SYNTHESIZE NUCLEOSIDE MONO-, DI- AND TRIPHOSPHATES IN WHICH ONE OF THE OXYGENS OF \, A OR G PHOSPHORUS HAS BEEN REPLACED WITH AN ISOELECTRONIC BORANE GROUP. THESE COMPOUNDS MAY BE PREPARED BY PHOSPHORYLATION OF NUCLEOSIDES, NUCLEOSIDE MONOPHOSPHATES AND NUCLEOSIDE DIPHOSPHATES USING A BORONATED PHOSPHORYLATING AGENT. IN OUR STUDIES WITH RELATED OLIGONUCLEOTIDE BORANOPHOSPHATES, THE P-BH3 MOIETY HAS BEEN FOUND TO BE REMARKABLY STABLE AND THE OLIGONUCLEOTIDE BORANOPHOSPHATES HAVE HIGH NUCLEASE RESISTANCE. THE NUCLEOSIDE BORANOPHOSPHATES MAY BE USEFUL IN A NUMBER OF WAYS INCLUDING: 1) AS TOOLS FOR STUDYING MECHANISM OF ACTION OF ENZYMES, 2) AS ANTIVIRAL AND ANTITUMOR AGENTS, AND 3) AS CARRIERS OF BORON FOR BORON NEUTRON CAPTURE THERAPY.

* information listed above is at the time of submission.

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