Boronated Nucleoside Bases

Award Information
Agency:
Department of Health and Human Services
Branch
n/a
Amount:
$50,000.00
Award Year:
1993
Program:
SBIR
Phase:
Phase I
Contract:
n/a
Award Id:
22031
Agency Tracking Number:
22031
Solicitation Year:
n/a
Solicitation Topic Code:
n/a
Solicitation Number:
n/a
Small Business Information
620 Hutton Street, Suite 104, Raleigh, NC, 27606
Hubzone Owned:
N
Minority Owned:
N
Woman Owned:
N
Duns:
n/a
Principal Investigator:
Bernard F. Spielvogel
(919) 832-2044
Business Contact:
() -
Research Institution:
n/a
Abstract
We will design and synthesize novel nucleic acid base derivatives containing cyanoborane group attached to a pyridine-type nitrogen atom of the purine or the pyrimidine cycle. The cyanoboronated bases may be designed to be more membrane soluble than the respective 2'- deoxyribonucleosides of known cytotoxic activities. In living organisms, these base derivatives may be converted to the 5'-nucleotides according to salvage pathways, even in cases when the respective 2'- deoxyribonucleosides are poor substrates for nucleoside kinases. Therefore, the cyanoboronated bases are expected to show better cytotoxic activities than the cyanoboronated 2'-deoxyribonucleosides and are feasible to use as antineoplastic agents. An additional importance is the potential for the compounds to be used in boron neutron capture therapy for the treatment of cancer. A rationale for the general synthetic approach to cyanoboronated nucleic acid bases is presented.

* information listed above is at the time of submission.

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