1992 Fiscal Year Final Research Report Summary
Molecular design and synthesis of new retinoids
| Project/Area Number |
02557084
|
|---|
| Research Category |
Grant-in-Aid for Developmental Scientific Research (B)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
Chemical pharmacy
|
|---|
| Research Institution | Univ. of Tokyo |
|---|
Principal Investigator |
SHUDO Koichi Univ. Tokyo, Prof., 薬学部, 教授 (50012612)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
KAGECHIKA Hiroyuki Univ. Tokyo Assist Prof., 薬学部, 助手 (20177348)
OHWADA Tomohiko Univ. Tokyo, Assist Prof., 薬学部, 助手 (20177025)
|
|---|
| Project Period (FY) |
1990 – 1992
|
| Keywords | retinoid / vitamin A / retinoic acid / retinoid antagonist / cancer / leukemia / differentiation / retinoid receptor |
|---|
| Research Abstract |
Molecular design ant synthesis of retinoids were practiced toward possible therapeutic applications.
1. New retinoids containing a trimethylsilyl or trimethylgermyl moiety were prepared. Some of them are very stong in the differentiation inducing bioassay.
2. Trans amide conformation of some synthetic retinoids is proved more important for the strong biological activity.
3. Retinoid receptors were expressed in animal cells and also in E. Coli. Using these receptors binding constants of several synthetic retinoids were evaluated.
4. Fluorescent retinoid probes were prepared.
5. Retinoid antagonists were synthesized for the first time.
6. An in vitro cancerstatic activity was tested using a malignant transformation model.
7. Three retinoid symposiums were held during the term, where some of the results were presented.
|
Research Products
(16 results)
