2013 Fiscal Year Final Research Report
Design and synthesis of novel vitamin D receptor ligands having a functional group that reinforces the interaction with the receptor
| Project/Area Number |
23590142
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | Tokushima Bunri University |
|---|
Principal Investigator |
|
|---|
| Project Period (FY) |
2011 – 2013
|
| Keywords | ビタミン / ホルモン / 核内受容体 / ステロイド / 化学合成 |
|---|
| Research Abstract |
Novel vitamin D receptor (VDR) ligands having a functional group designed to reinforce the interaction to the VDR through a certain amino acid residue were synthesized. The ligands having a carboxy group in the A-ring of vitamin D instead of the important 1alpha-hydroxy group were synthesized by a convergent method using palladium catalyst. In addition, vitamin D analogues having a spiro-oxetane fused at the C2 position in the A-ring were also synthesized. The VDR binding of the synthesized compounds revealed that the introduction of a carboxy group or an oxetane into the C2 position of the A-ring would compensate the loss of the 1alpha-hydroxy group to a certain extent to generate unique vitamin D analogues.
|
