| Project/Area Number |
25670060
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Kitasato University |
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Principal Investigator |
INUI Hiroshi 北里大学, 理学部, 講師 (20348600)
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| Project Period (FY) |
2013-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥3,380,000 (Direct Cost: ¥2,600,000、Indirect Cost: ¥780,000)
Fiscal Year 2014: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2013: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 光反応 / ドキシフルリジン / 抗癌剤 / プロドラッグ / 光分解性保護基 |
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| Outline of Final Research Achievements |
In cancer therapy, the ability to destroy tumor tissue rather than normal tissue is important for reducing side effect. To achieve this goal, I developed photoactivated anticancer prodrugs to release doxifluridine (DF). Photoreactions allow a reaction to be induced the desired time and space through the control of irradiation conditions. DF is known to undergo conversion to cytotoxic 5-fluorouracil catalyzed by an enzyme, which is more highly expressed in cancer cells than in normal ones. Therefore, the combination of this high-priority DF conversion in cancer cells with the target selectivity of photoreaction should lead to a further decrease of the side effects. In this work, photochemical DF donors having a newly developed nitroquinolyl protecting group were synthesized, and the photoreactivity were compared to that of other DF donors possessing the widely used 2-nitrobenzyl groups. Furthermore, the behavior of the DF donors in living cells and their cytotoxicity were investigated.
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