1995 Fiscal Year Final Research Report Summary
Studies on specific structure of 4'-thionucleosides and the molecular recognition by kinases.
| Project/Area Number |
06455020
|
|---|
| Research Category |
Grant-in-Aid for General Scientific Research (B)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
広領域
|
|---|
| Research Institution | Okayama University of Science |
|---|
Principal Investigator |
UENISHI Junichi Okayama University of Science, Faculty of Science Professor, 理学部, 教授 (50167285)
|
|---|
| Project Period (FY) |
1994 – 1995
|
| Keywords | 4'-thionucleic acid / 4-thiofuranose / anti-HIV activity / anti-HSV activity / cytotoxicity / stereoselective synthesis |
|---|
| Research Abstract |
Chemical modification of the sugar moiety in nucleoside is one of the promising way to find a new chemotherapeutic agent. Nucleoside possessing a heterocyclic ring instead of 2-deoxyribose or ribose is so called pseudo nucleoside. Since HIV (human immunodeficiency virus) has appeared to cause the serious disease in the human life, such nucleosides have received considerable attentions as a new anti-viral medicine. Synthesis and biological study of 4'-thio nucleoside in which furanose ring oxygen atom is replaced by a sulfur atom, is a main purpose of this research. During the investigation, a general synthetic method of 2'-deoxy-4'-thioribonucleosides was established under acyclic stereocontrol. Examination of anti-viral activity revealed that 4'-thiothimidine and 2'-deoxy-4'-methyl-4'-thiocytidine have anti-HIV activity as potent as AZT.They were also very effective against HSV-1 and HSV-2 at lower than 0.3 mug/mL level (IC50). Particularly, 4'-methyl-4'-thiothimidine inhibited 50% growth of HSV-1 at 0.04 mug/mL concentration.
|
