Abstract

This proposal is a request for funding to study the total synthesis of the recently discovered antitumor antibiotic quinocarcin (1,DC-52). Being the simplest member of the saframycin/naphthyridinomycin class of antibiotics, the synthetic protocol developed will focus on the asymmetric preparation of the isoquinoline nuclei and the bicyclic piperazines such that synthetic entries to naphthyridinomycin will be realized. It is the purpose of this proposal to establish the functional significance of the bicyclic piperazine moiety in imparting chemical stability manifested as biological reactivity in the DC-52 molecule. A mechanism of action is proposed and synthetic protocol will be established to probe both the covalent modification of DNA as well as the reported oxygen-dependent DNA strand scission by DC-52.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Research Project (R01)
Project #
5R01CA043969-02
Application #
3186480
Study Section
Medicinal Chemistry Study Section (MCHA)
Project Start
1987-01-01
Project End
1989-12-31
Budget Start
1988-01-01
Budget End
1988-12-31
Support Year
2
Fiscal Year
1988
Total Cost
Indirect Cost

  Institution

Name
Colorado State University-Fort Collins
Department
Type
Schools of Arts and Sciences
DUNS #
112617480
City
Fort Collins
State
CO
Country
United States
Zip Code
80523