2010 Fiscal Year Final Research Report
Small molecular library of alpha-fluorinated and -hydroxylated carbonyl compounds synthesized by newly developed reactions
| Project/Area Number |
20590114
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Matsuyama University |
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Principal Investigator |
KAWASE Masami Matsuyama University, 薬学部, 教授 (20112641)
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| Co-Investigator(Kenkyū-buntansha) |
HAGIMOTO Yuri 松山大学, 薬学部, 講師 (30435078)
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| Co-Investigator(Renkei-kenkyūsha) |
SAKAGAMI Hiroshi 明海大学, 歯学部, 教授 (50138484)
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| Project Period (FY) |
2008 – 2010
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| Keywords | 化合物ライブラリー / カルボニル化合物 / トリフルオロメチルケトン / クロロジフルオロメチルケトン / ヒドロキシケトン / アポトーシス / オートファジー / クオラムセンシング |
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| Research Abstract |
A novel transformation of N-acylprolines to enol esters was realized by utilizing chlorodifluoroacetic or trifluoroacetic anhydrides in the presence of inorganic bases. Mesoionic 4-trifluoroacetyl-1,3-oxazolium-5-olates reacted with phosphorus-ylides to give 3(beta)-trifluoromethylpyrroles in good yields. Biological results : Screenings of a variety of structurally diverse ketones led to the identification of several apoptosis- and autophagy-inducers and quorum sensing (QS) inhibitors of alpha-trifluoromethylacyloins, N-acyl-1,2,3,4-tetrahydroisoquinolines, and 2-trifluoroacetonylbenzoxazoles as a lead molecule.
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[Journal Article] 2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides : A Novel Cluster of Tumor-specific Cytotoxins which Reverse Multidrug Resistance.2009
Author(s)
U.Das, H.N.Pati, A.K.Panda, E.De Clercq, J.Balzarini, J.Molnar, Z.Barath, I.Ocsovzki, M.Kawase, H.Sakagami, J.R.Dimmock
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Journal Title
Bioorg.Med.Chem. 17
Pages: 3909-3915
Peer Reviewed
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[Journal Article] Tumor-specific Cytotoxic Activity of 1,2,3,4-Tetrahydroisoquinoline Derivatives against Human Oral Squamous Cell Carcinoma Cell Lines.2009
Author(s)
H.Hatano, H.Takekawa, K.Hashimoto, M.Ishihara, M.Kawase, C.Qing, W.Qin-Tao, H.Sakagami
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Journal Title
Anticancer Res. 29
Pages: 3079-3086
Peer Reviewed
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