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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 35, Number 8
BKCSDE 35(8)
August 20, 2014 

Synthesis and Anticancer Activity of Some Novel 1,3-Diaryl/heteroarylprop-2-en-1-one Derivatives
Mayank Kinger, Jeong Hoon Park, Jun Young Lee, Sang Wook Kim*
1,3-Diaryl/heteroarylprop-2-en-1-one, Pyrazole, Anti-cancer, Reactive oxygen species
In the present investigation, a series of some novel 1,3-diaryl/heteroarylprop-2-en-1-one derivatives (3a-j) have been synthesized and evaluated for their in vitro cytotoxicity against three cancer cell lines, two hepatocarcinoma cell lines HUH-7, Hep-3b and one leukemia cancer cell line MOLT-4. Based on these results, structure-activity relationship (SAR) was studied on modification of R1 and R2 to identify the compound with maximum potency. Amongst the compounds, 3b and 3d strongly inhibited the growth of Hep-3b and MOLT- 4 cells with IC50 value of 3.39 and 3.63 μM respectively. The results obtained from the inhibitory study had further been supported by the reactive oxygen species (ROS) measurement using flow cytometry in MOLT-4 cells. These observations collectively reveal that compounds comprising 1,3-diarylprop-2-en-1-one framework with pyrazole ring at position-3 and heteroaryl/aryl substituents at position-1 can be used as promising anticancer agents.
2375 - 2380
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