| title: | Annonaceous acetogenin analogs: synthesis and its biological and physical properties |
|---|---|
| reg no: | ETF6520 |
| project type: | Estonian Science Foundation research grant |
| status: | accepted |
| institution: | University of Tartu |
| head of project: | Lauri Vares |
| duration: | 01.01.2005 - 31.12.2008 |
| description: | Annonaceous acetogenins are a relatively new class of naturally occurring bioactive compounds. Chemically, they are derivatives of long chain fatty acids, with tetrahydrofuran (THF) and butenolide moieties as common structural features. They offer wide range of biological activities such as anthelmintic, antimalarial, antimicrobial, antiprotozoal, and cytotoxic antitumor, and they show a special promise for becoming a new type of antitumor and pesticidal agents. In this project new type of simplified acetogenin analogs will be synthesized (e.g. bis-THF units will be replaced ethyl diamine or/and ethyl disulfide units). Synthetic methodology will be chosen so that it will enable the synthesis of many close analogs in parallel format. Testing the biological activity of close analogs will give a new valuable information about the structure-activity relationship (SAR). In addition, complexation studies with different cations (Ca2+, Ba2+, K+) will be carried out by using NMR spectroscopy. Cations have an important role in acetogenins mode of action and the complexation has therefore directly connected with activity. The potential use of such acetogenin analogs in therapeutic uses and as novel ionophores will be studied. |
| project group | ||||
|---|---|---|---|---|
| no | name | institution | position | |
| 1. | Lauri Vares | University of Tartu | Researcher | |