| Summary: | 碩士 === 大仁科技大學 === 製藥科技研究所 === 98 === Certain oxime-containing 3,4-dihydroquinolin-2(1H)-one derivatives
were synthesized and evaluated for their antiplatelet and antiproliferative
activities. These compounds were synthesized via alkylation of hydroxyl precursors followed by the reaction with NH2OH .
The preliminary assays indicated that (Z)-7-(2-(4-fluorophenyl)-2-(h
ydroxyimino)ethoxy)-3,4-dihydroquinolin-2(1H)-one (13c) was the most
active against U46619 induced platelet aggregation with an IC50 value of 3.51 μM. For the inhibition of AA-induced aggregation, (E)-6-(2-(hydrox
yimino)propoxy)-3,4-dihydroquinolin-2(1H)-one (15) was the most potent
with an IC50 value of 1.85 μM. These oxime-containing 3,4-dihydroquino
lin-2(1H)-one derivatives were inactive against thrombin induced platelet
aggregation with an IC50 value of greater than 26.78 μM. For the
antiproliferative activity, most of these oxime-containing 3,4-dihydroquin
olin-2(1H)-one derivatives were inactive while (Z)-7-(2-(hydroxyimino)-
2-(naphthalen-2-yl)ethoxy)-3,4-dihydroquinolin-2(1H)-one (13a)
exhibited only marginal activities with IC50 value of 7.63, 7.34 and 6.36
μM against the growth of NPC-TW01, H-661, and Jurkat respectively.
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