2013 Fiscal Year Final Research Report
Synthesis the naphto[1,8-bc]furan and polycyclic heterocycles with good bioactivity.
| Project/Area Number |
23590143
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Health Sciences University of Hokkaido (2012-2013)
Matsuyama University (2011) |
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Principal Investigator |
HATAE Noriyuki 北海道医療大学, 薬学部, 准教授 (30449912)
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| Co-Investigator(Kenkyū-buntansha) |
HIBINO Satoshi 福山大学, 薬学部, 教授 (60112885)
CHOSHI Tominari 福山大学, 薬学部, 教授 (10248297)
ISHIKURA Minoru 北海道医療大学, 薬学部, 教授 (10146011)
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| Project Period (FY) |
2011 – 2013
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| Keywords | ナフト[1,8-bc]フラン / 分子内Diels-Alder反応 / ハロゲン化ジエン / アレニルエーテル / 抗腫瘍活性物質 / calothrixin / 生物活性物質 |
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| Research Abstract |
Polycyclic heterocycles were known as the privileged compound, and their structural features were consisted rigid conforamation and were highly-reactive to the biomolecules. It was extremely difficult for the synthesis of the compounds because of their high-reactivity. Particularly, the naphto[1,8-bc]furan ring system was consisted a lot of enzyme inhibitors, such as wortomanin, halenaquinone and xestoquinone. A convinced synthetic route for the core ring system was developed by tandem [4+2] cycloaddition/aromatization sequence of allenyl 2-halo-3-vinylcyclohex-2-enyl ethers. Furthermore, the antiproliferative activity by the polycyclic heterocycles was identified.
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[Journal Article] Effects of 1,3-di-O- substituted myo-inositol derivatives on the antiproliferation and caspase-3 activity of HCT- 116 and HL-60 cells2014
Author(s)
Noriyuki Hatae, Satoe Yamauchi, Takafumi Saeki, Ichiro Suzuki, Tominari Choshi, Satoshi Hibino, Chiaki Okada, Minoru Hayashi, Yutaka Watanabe, Eiko Toyota
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Journal Title
Chem Biol Lett
Volume: 1
Pages: 40-43
URL
Peer Reviewed
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[Journal Article] Synthesis of 4-arylpiperidin-4-ol derivatives of loperamide as agents with potent antiproliferative effects against HCT-116 and HL-60 cells2014
Author(s)
Noriyuki Hatae, Tomoyuki Nagayama, Hiroyoshi Esaki, Eiko Kujime, Masabumi Minami, Minoru Ishikura, Tominari Choshi, Satoshi Hibino, Chiaki Okada, Eiko Kujime, Hideko Nagasawa, Tatsunori Iwamura
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Journal Title
Heterocycles
Volume: 88
Pages: 663-673
DOI
Peer Reviewed
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[Journal Article] Effects of the orthoquinone moiety in 9,10- phenanthrenequinone on its ability induce apoptosis in HCT-116 and HL-60 cells2013
Author(s)
Noriyuki Hatae, Jun Nakamura, Tetsuo Okujima, Minoru Ishikura, Takumi Abe, Satoshi Hibino, Tominari Choshi, Chiaki Okada, Hiroko Yamada, Hidemitsu Uno, Eiko Toyota
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Journal Title
Bioorg Med. Chem. Lett
Volume: 23
Pages: 4637-4640
DOI
Peer Reviewed
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[Journal Article] N- substituted calothrixin B derivatives inhibited the proliferation of HL-60 promyelocytic leukemia cells
Author(s)
Noriyuki Hatae, Risa Satoh, Hitomi Chiba, Takahiro Osaki, Takashi Nishiyama, Minoru Ishikura, Takummi Abe, Satoshi Hibino, Tominari Choshi, Chiaki Okada, Eiko Toyota
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Journal Title
Med. Chem. Res
Volume: (in press)
Peer Reviewed
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