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BORONATED NITROIMIDAZOLES FOR NEUTRON CAPTURE THERAPY

Award Information

Agency:
Department of Energy
Branch:
N/A
Award ID:
11591
Program Year/Program:
1990 / SBIR
Agency Tracking Number:
11591
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
Karkinos Biochem Inc
4636 East Elwood Street #6 Phoenix, AZ 85040
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Woman-Owned: Yes
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 1990
Title: BORONATED NITROIMIDAZOLES FOR NEUTRON CAPTURE THERAPY
Agency: DOE
Contract: N/A
Award Amount: $50,000.00
 

Abstract:

BORON NEUTRON CAPTURE THERAPY (BNCT) USING THE (10)B(N, ALPHA)(7) LI REACTION OFFERS PROMISE AS A METHOD FOR SELECTIVE INTERNAL IRRADIATION OF TUMORS. (10)B-SUBSTITUTED AMINO ACIDS, NUCLEOSIDES, AND ANTIBODIES HAVE BEEN DEVELOPED TO TARGET TUMORS. RECENTLY, EXCITING DATA HAS BEEN GENERATED WITH BORONATED PORPHYRINS AND CAGED DODECABORANE SULFHYDRYL COMPOUNDS AS BNCT AGENTS. SINCE EFFECTIVE BNCT MAY ULTIMATELY REQUIRE "COCKTAILS" OF (10)B CARRIERS FOR BEST THERAPEUTIC RESPONSES, THERE IS A NEED FORCONTINUED DEVELOPMENT OF (10)B CARRIERS. IN THIS PHASE I SBIR PROJECT, WE PROPOSE THE DEVELOPMENT OF BORONATED NITROIMIDAZOLES AS BNCT AGENTS. THIS CLASS OF AGENT IS KNOWN TO EFFECTIVELY PENETRATE SOLID TUMORS AT MILLIMOLAR LEVELS NECESSARY FOR BNCT, AND TO UNDERGO REDUCTIVE METABOLISM TO DNA- AND PROTEIN-BOUND FORMS. THIS PROPOSAL IS COMPOSED OF 5 TASKS: 1) SYNTHESIS OF A MONOBORONATED METRONIDAZOLE MIMIC WITH NATURAL ABUNDANCE BORON; 2) SYNTHESIS OF THE MONOBORONATED AGENT WITH (10)B; 3) SYNTHESIS OF A (10)B-DO-DECABORONATED METRONIDAZOLE DERIVATIVE; 4) TESTING OF COMPOUNDS IN 2) AND 3) FOR ACTIVITY IN A V-79 CELL-BASED IN VITRO BNCT PROTOCOL, WHICH INCLUDES EVALUATION OF CELL UPTAKE; 5) PRELIMINARY EVALUATION OF THE UPTAKE AND DISTRIBUTION OF COMPOUNDS IN 1) AND 3) BY C57B1/6 MICE BEARING THE COLON 38 TUMOR MODEL. THESE STUDIES ARE DESIGNED TO EVALUATE THE FEASIBILITY OF BORONATED NITROIMIDAZOLES AS POTENTIAL BNCT AGENTS BASED THE ASSAYS IN 4) AND 5), AND ALSO WILL GIVE AN INDICATION OF THE EFFECTS OF A LOWER LIMIT (MONO) AND AN UPPER LIMIT (DODECA) OF BORONATION ON THE BEHAVIOR OF THIS CLASS OF AGENT.

Principal Investigator:


0

Business Contact:

David h. swenson
PRESIDENT
6028942528
Small Business Information at Submission:

Karkinos Biochem Inc
4636 East Elwood Street #6 Phoenix, AZ 85040

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