Kadsurenone, a constituent of the Chinese herbal plant Piper futokadsura (heifenteng) is a potent and specific platelet activating factor (PAF) antagonist. A short and efficient synthesis of Kadsurenone is being developed. Experience gained in this work will be used to synthesize mirestrol, a naturally occurring estrogen. Pilocarpine is a clinically used antiglaucoma agent. It is presently isolated from Pilocarpus jaborandi, a rapidly disappearing tropical tree. A total synthesis of enantiomerically and stereochemically pure pilocarpine is under investigation. Vinblastine and vincrystine are useful but very expensive antitumor agents. A new synthetic scheme from natural vindoline and a totally synthetic component will be tested experimentally. Alchorneine and isoalchorneine, two methoxyguanidine alkaloids are used in Central African folk medicine for various ailments. The two agents do not seem to have been examined by modern pharmacological methods. Work on total syntheses has been initiated.

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Research Project (R01)
Project #
2R01GM009686-26
Application #
3268039
Study Section
Medicinal Chemistry Study Section (MCHA)
Project Start
1977-04-01
Project End
1990-03-31
Budget Start
1987-04-01
Budget End
1988-03-31
Support Year
26
Fiscal Year
1987
Total Cost
Indirect Cost
Name
Massachusetts Institute of Technology
Department
Type
Schools of Arts and Sciences
DUNS #
City
Cambridge
State
MA
Country
United States
Zip Code
02139