Unified Total Synthesis and Structure-Activity Relationships of Marine Macrolide Natural Products of Cyanobacteria Origin
| Project/Area Number |
23681045
|
|---|
| Research Category |
Grant-in-Aid for Young Scientists (A)
|
| Allocation Type | Single-year Grants |
|---|
| Research Field |
Living organism molecular science
|
|---|
| Research Institution | Tohoku University |
|---|
Principal Investigator |
FUWA Haruhiko 東北大学, 生命科学研究科, 准教授 (90359638)
|
|---|
| Project Period (FY) |
2011-04-01 – 2014-03-31
|
| Project Status |
Completed (Fiscal Year 2013)
|
| Budget Amount *help |
¥26,000,000 (Direct Cost: ¥20,000,000、Indirect Cost: ¥6,000,000)
Fiscal Year 2013: ¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2012: ¥7,930,000 (Direct Cost: ¥6,100,000、Indirect Cost: ¥1,830,000)
Fiscal Year 2011: ¥12,610,000 (Direct Cost: ¥9,700,000、Indirect Cost: ¥2,910,000)
|
|---|
| Keywords | 海洋天然物 / 全合成 / 構造活性相関 / 生物活性分子の設計 / 細胞増殖阻害 / ミトコンドリア / 作用解析 / 抗がん作用 / マクロリド |
|---|
| Research Abstract |
This project pursued unified total synthesis and structure-activity relationships of marine macrolide natural products of cyanobateria origin. Our concise synthesis of neopeltolide, a highly potent antiproliferative macrolide, enabled us to elucidate its pharmacophoric structural elements required for potent activity. Several truncated neopeltolide analogues with nanomolar activity were successfully designed on the basis of our pharmacophore model. Concise total synthesis of lyngbyaloside B, a moderately cytotoxic macrolide glycoside, and its 13-demethyl analogue was also achieved. Design, synthesis, and biological evaluation of chimeric macrolides were undertaken to show that polyketide macrolides offer unique structural motifs useful for the development of novel antiproliferative agents.
|
Report
(4 results)
Research Products
(74 results)
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
[Journal Article] Design and synthesis of skeletal analogues of gambierol : Attenuation of amyloid-βand tau pathology with voltage-gated potassium channel and N-methyl-D-aspartate receptor implications2012
Author(s)
E. Alonso, H. Fuwa, C. Vale, Y. Suga, T. Goto, Y. Konno, M. Sasaki, F. M. LaFerla, M. R. Vieytes, L. Gimenez-Llort, L. M. Botana
-
Journal Title
J. Am. Chem. Soc
Volume: 134
Issue: 17
Pages: 7467-7479
DOI
Related Report
Peer Reviewed
-
-
-
-
[Journal Article] Comparative cytotoxicity of gambierol versus other marine neurotoxins2011
Author(s)
E.Cagide, M.C.Louzao, B.Espina, I.R.Ares, M.R.Vieytes, M.Sasaki, H.Fuwa, M.Yotsu-Yamashita, L.A.Paquette, T.Yasumoto, L.M.Botana
-
Journal Title
Chemical Research in Toxicology
Volume: 24
Issue: 6
Pages: 835-842
DOI
Related Report
Peer Reviewed
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
