Li-Chai Chen, I‐Li Chen, Chih-Chiang Huang
Dec 1, 2010
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0
Influential Citations
3
Citations
Quality indicators
Journal
Journal of The Chinese Chemical Society
Abstract
Some 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 NH 2 OH. The preliminary assays indicated that (Z)-7-[2-(4-fluorophenyl)-2-(hydroxyimino)ethoxy]-3,4-dihydroquino)in-2(1H)-one (13c) is the most active against U46619 induced platelet aggregation with an IC 50 value of 3.51 μM. For the inhibition of AA-induced aggregation, (E)-6-[2-(hydroxyimino)propoxy]-3,4-dihydroquinolin-2(1H)-one (15) is the most potent with an IC 50 value of 1.85 μM. These oxime-containing 3,4-dihydroquinolin-2(1H)-one derivatives were inactive against thrombin induced platelet aggregation with an IC 50 value of greater than 26.78 μM. For the antiproliferative activity, most of these oxime-containing 3,4-dihydroquinolin-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 GI 50 value of 7.63, 7.34 and 6.36 μM against the growth of NPC-TW01, NCI-H661, and Jurkat respectively.