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Amine-Boranes as New Topoisomerase II Inhibitors

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
21967
Program Year/Program:
1993 / SBIR
Agency Tracking Number:
21967
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
BORON BIOLOGICALS, INC.
620 HUTTON ST, STE 104 RALEIGH, NC 27606
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Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 1993
Title: Amine-Boranes as New Topoisomerase II Inhibitors
Agency: HHS
Contract: N/A
Award Amount: $50,000.00
 

Abstract:

The main objective of the research is to develop a new class of topoisomerase II (Topo II) inhibitors as antineoplastic agents. In preliminary studies, heterocyclic amine-carboxyboranes have been shown to possess cytotoxic activity against a number of murine and human tumor tissue culture lines, e. g. P388, L1210, Tmolt3, HeLa-S3, lung bronchogenic, KB nasopharynx, glioma, and osteosarcoma. These compounds have been shown to inhibit HeLa-S3 Topo II at 100 mu M concentration, but have not been tested below this concentration. The Phase I objectives are to synthesize a larger selection of amine-carboxyboranes and to evaluate the effect of Lewis base moiety on biological activity. Studies will be performed to determine in vitro cytotoxicity and in vivo antitumor activity of these compounds. Mode of action studies will be limited to Topo II inhibition, inhibition of DNA synthesis, and DNA stability in Phase I. Phase II studies will concentrate further on structure-activity relationship with the help of molecular modeling. In addition, detailed mode of action, acute toxicity, tissue disposition, and pharmacokinetic parameters will be determined. The project is expected to result in the identification and development of one or more potent antineoplastic agents to treat one or more human tumors.

Principal Investigator:

Bernard F. Spielvogel
9198322044

Business Contact:

Small Business Information at Submission:

Boron Biologicals, Inc.
620 Hutton Street, Suite 104 Raleigh, NC 27606

EIN/Tax ID:
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No