Characterization and application of hydrophobic functionalities bearing heavier group 14 atoms
| Project/Area Number |
23790128
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo Medical and Dental University |
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Principal Investigator |
FUJII Shinya 東京医科歯科大学, 生体材料工学研究所, 助教 (60389179)
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| Project Period (FY) |
2011 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Fiscal Year 2011: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 医薬品化学 / 疎水性相互作用 / 有機元素化学 / エストロゲン / 定量的構造活性相関 / 疎水性 / ケイ素 / ゲルマニウム / 分配係数 / 構造活性相関 |
|---|
| Research Abstract |
Systematic synthesis and characterization of simple phenols bearing a trialkyl(aryl)silyl or trialkyl(aryl)germyl functional group as a hydrophobic substituent were investigated. These silicon and germanium analogs exhibited higher hydrophobicity than the corresponding carbon analogs, with a difference in logP value of approximately 0.6, independent of the alkyl(aryl) species. The trialkylsilyl- and trialkylgermylphenols exhibited more potent estrogenic activity as compared with the carbon analogs. The substituent parameters and structure-activity relationship may be helpful for drug discovery utilizing the heavier group 14 elements.
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Report
(3 results)
Research Products
(51 results)
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[Journal Article] Boron Cluster-based DevNon-Secosteroidal Vitamin D Receptor Ligands: Direct Observation of Hydrophobic Interaction between Protein Surface and Carborane2011
Author(s)
Shinya Fujii, Hiroyuki Masuno, Yoshiyuki Taoda, Atsushi Kano, Angsuma Wongmayura, Makoto Nakabayashi, Nobutoshi Ito, Masato Shimizu, Emiko Kawachi, Tomoya Hirano, YasuyukiEndo, Aya Tanatani, Hiroyuki Kagechika
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Journal Title
J. Am. Chem. Soc
Volume: 133
Issue: 51
Pages: 20933-20941
DOI
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Peer Reviewed
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[Presentation] Novel non-secosteroidal vitamin D receptor ligands bearing a spherical hydrophobic core. - Difference between carborane and bicyclohydrocarbon -2011
Author(s)
Angsuma, W.; Fujii, S.; Sekine, R.; Kano, A.; Kawachi, E.; Masuno, H.; Hirano, T.; Kagechika, H.; Tanatani, A.
Organizer
IME Boron XIV
Place of Presentation
Niagara Falls, Canada
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[Presentation] Development of Novel AR Antagonists Active in LNCaP Cells with Mutated Androgen Receptor.2011
Author(s)
Yamada, A., Fujii, F., Tomita, K., Nagano, M., Harayama, T., Ohta, K., Endo, Y., Kagechika, H.
Organizer
AIMECS11
Place of Presentation
Tokyo
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