Amine-Boranes as New Topoisomerase II Inhibitors

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 21967
Amount: $50,000.00
Phase: Phase I
Program: SBIR
Awards Year: 1993
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
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 Bernard F. Spielvogel
 (919) 832-2044
Business Contact
Phone: () -
Research Institution
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.

* Information listed above is at the time of submission. *

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