| 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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| 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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