| Project/Area Number |
26460156
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | Tokyo University of Science |
|---|
Principal Investigator |
Aoki Shin 東京理科大学, 薬学部生命創薬科学科, 教授 (00222472)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
安部 良 東京理科大学, 研究推進機構生命医科学研究所, 教授 (20159453)
西道 隆臣 国立研究開発法人理化学研究所, 脳科学総合研究センター, チームリーダー (80205690)
小野 公二 京都大学, 原子炉実験所, 寄附研究部門教員 (90122407)
|
|---|
| Co-Investigator(Renkei-kenkyūsha) |
HISAMATSU YOSUKE 東京理科大学, 薬学部, 助教 (80587270)
|
|---|
| Project Period (FY) |
2014-04-01 – 2017-03-31
|
| Project Status |
Completed (Fiscal Year 2016)
|
| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2016: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2015: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2014: ¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000)
|
|---|
| Keywords | ホウ素中性子捕捉療法 / 天然物 / グルコサミン / ホウ素クラスター / 銅 / ホウ素 / キャリア / グルコース / 中性子捕捉療法 / NMR / MRI |
|---|
| Outline of Final Research Achievements |
Objective of this work is to deliver boron-containing compounds to tumor sites and to detect (visualize) the accumulation of boron in tumor size (in vivo imaging of boron compounds) for boron neutron capture therapy (BNCT). In this work, we have succeeded in the synthesis of sulfoquinovosylacyl-1,3-propanediol (SQAP) having a hydrophobic boron-containing alkyl group containing boron cluster for BNCT and iodo groups for computed tomography (CT). However, tumor accumulation of those SQAP derivatives were low and their toxicity to mouse was detected. Next, design and synthesis of sugar derivatives to target glucose transporters that are overexpressed on cancer cells were conducted. These D-glucosamine analogs are less toxic and some compounds exhibit fairly good T/B (tumor/blood) ratios. It was found that o-carborane undergoes decomposition in the presence of copper(II) ion in aqueous solution at neutral pH to generate 10 B(OH)3, which was applied to 11B MRI probe of Cu2+.
|
