Synthesis of anticanter 4-(1-anisoyl-1-hydroxyethyl)quinazolines and the elucidation of their action mechanism
| Project/Area Number |
24590140
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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 | Sophia University |
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Principal Investigator |
SUZUKI Yumiko 上智大学, 理工学部, 准教授 (20295546)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 合成化学 / 創薬化学 / 有機分子触媒 / 有機化学 / 抗がん / 抗がん剤 |
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| Outline of Final Research Achievements |
A series of anticancer quinazolines were synthesized and a dozen of new compounds were found to be several dozen times more active than the original hit, PVHD121. (+)-PVHD121 is more active than (-)-isomer. Their boromo-isomers PVHD121Brs were also prepared and separated. The stereochemical correlation between (+) and (-)-PVHD121 and (+) and (-)-PVHD121Br became clear. The most active racemate ever is PVHD303. Its enantiomers were separated and tested for their antiproliferative activity and one of them were ca. ten times active than the other. Bromo-substituted version of it, PVHD303Br was also synthesized and separated into enantiomers. X-ray crystallographic analysis of bromo-isomers would elucidate the absolute stereochemistries of the enantiomers ofPVHD121, PVHD121Br, PVHD303, PVHD303Br.
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Report
(4 results)
Research Products
(35 results)
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[Presentation] 求核的アシル化反応の開発研究2014
Author(s)
土橋滉平, 岩田直人, 石坪江梨香, 常盤広明, 鈴木由美子
Organizer
CSJ化学フェスタ
Place of Presentation
タワーホール船堀（東京都、江戸川区）
Year and Date
2014-10-16
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