Synthesis and Anticancer Activity of Some Novel 1,3-Diaryl/heteroarylprop-2-en-1-one Derivatives

Bulletin of the Korean chemical society

Mayank Kinger¹  Jeong Hoon Park¹  Sang Wook Kim¹  Jun Young Lee¹ 

关键词: 1;    3-Diaryl/heteroarylprop-2-en-1-one;    Pyrazole;    Anti-cancer;    Reactive oxygen species;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown