| Project/Area Number |
01571161
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| Research Category |
Grant-in-Aid for General Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Research Field |
Chemical pharmacy
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| Research Institution | KITASATO UNIVERSITY |
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Principal Investigator |
ZEN SHONOSUKE KITASATO UNIV., Pharmaceutical Sci., Professor, 薬学部, 教授 (80050342)
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| Co-Investigator(Kenkyū-buntansha) |
HIROTANI SEIKO KITASATO UNIV., Pharmaceutical Sci., Assistant, 薬学部, 助手 (20050594)
HIROOKA MOTOKO KITASATO UNIV., Pharmaceutical Sci., Assistant, 薬学部, 助手 (20050578)
HARADA KAZUHO KITASATO UNIV., Pharmaceutical Sci., Assistant, 薬学部, 助手 (00189698)
KAJI EISUKE KITASATO UNIV., Pharmaceutical Sci., Lecturer, 薬学部, 講師 (60050598)
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| Project Period (FY) |
1989 – 1990
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| Project Status |
Completed (Fiscal Year 1990)
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| Budget Amount *help |
¥600,000 (Direct Cost: ¥600,000)
Fiscal Year 1990: ¥600,000 (Direct Cost: ¥600,000)
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| Keywords | Bisintercalator / Oligonucleotide / Pyridocarbazole / Ring transformation |
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| Research Abstract |
With the aim of developing a novel type of anticancer alkylating agents, e.g. oligonucleotides bearing two intercalator groups (1), Synthetic routes of ellipticine (2), 9-hydroxyellipticine (3), and 11-fluoromethyl-9-hyaroxy-5-methy1-6H-pyrido[4,3-b]carbazole (4) was investigated in the following manners.
1) Ellipticine (2) was synthesized starting from 3-ethyl-4-methylpyridine. 9-Hydroxyellipticine (3) was also attempted to synthesize in a similar manner, however, there are several steps to compete the total synthesis of 3.
2) In the case of total synthesis of 4, the key compound, pyrido[4,3-b]-carbazole dervative (6), was obtained in six steps starting from 5- methoxyindole.
3) Another approach to synthesize 4 employing the ring transformation of isoxazoline N-oxide to 3H--indole was investigated. In the course of this project, we found several new ring transformations of isoxazoline Nーoxide.
4) The sugar moiety (5) was prepared and the synthesis of oligoncleotides by the condensation of these intercalators with 5 will be investigated.
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