| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2010: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Research Abstract |
To discover and develop lead-compounds for new antitumor medicines originated from plant alkaloids, chemical investigation and biological evaluation of Gelsemium alkaloids and colchicinoids were carried out. As results, several novel alkaloids were isolated from Gelsemium plants. Key intermediates of sarpagine-type alkaloids, one of the members of Gelsemium alkaloids, were synthesized utilizing gold-catalyzed cyclization. 4-Halocolchicines and 4-chlorocolchicine derivatives bearing anα-hydroxyacetoamide side chain at C-7 were found to show potent antitumor activities. Pro-drugs of highly-active colchicine derivatives were prepared and their selective toxicity to the tumor cells was evaluated.
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