The principal objectives of the next grant period are: (1) Continued development of efficient synthetic pathways for the mitomycins, FR-900482, and their epoxide analogs. These compounds are expected to show antitumor activities by cross-linking DNAs. (2) Completion of the total syntheses of discorhabdins A and C, unique marine natural products with antitumor activity. (3) Development of an efficient synthetic route for an antitumor antibiotic (-)-safracin B, which is amenable to preparation of a variety of analogs. (4) Efficient synthesis of oligothiazoline-type natural products including thiangazole, didehydromirabazole A, and their analogs. These compounds belong to a completely new family of biologically active compounds.It is hoped that compounds prepared from this project would exhibit unique antitumor and/or anti-HIV activities. (5) Development of an efficient synthetic protocol for indole alkaloids including tabersonine and catharanthine. Efficient synthesis of catharanthine and its analogs will enable the preparation of a variety of hitherto inaccessible analogs of vinblastine, a potent antitumor agent currently used clinically. (6) Completion of the total synthesis of gelsemine, a synthetically challenging alkaloid with CNS activity.

Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Research Project (R01)
Project #
2R01CA028119-15
Application #
2087697
Study Section
Bio-Organic and Natural Products Chemistry Study Section (BNP)
Project Start
1980-07-01
Project End
1999-12-31
Budget Start
1995-01-09
Budget End
1995-12-31
Support Year
15
Fiscal Year
1995
Total Cost
Indirect Cost
Name
Rice University
Department
Chemistry
Type
Schools of Arts and Sciences
DUNS #
050299031
City
Houston
State
TX
Country
United States
Zip Code
77005