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Molecules 2012, 17(6), 6179-6195; doi:10.3390/molecules17066179
Article

Synthesis of Chalcones with Anticancer Activities

1
,
2,* , 3
 and
4
1 UPM-MAKNA Cancer Research Lab, Institute of Bioscience, University Putra Malaysia, 43400 Serdang, Selangor, Malaysia 2 Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia 3 Department of Chemistry, Faculty of Science and Arts in Al-Mukhwah, Al-Baha University, Al-Baha 65431, Saudi Arabia 4 Centre for Natural Products and Drug Discovery (CENAR), Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia
* Author to whom correspondence should be addressed.
Received: 28 March 2012 / Revised: 20 April 2012 / Accepted: 27 April 2012 / Published: 25 May 2012
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Abstract

Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer) and human normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC50 values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p < 0.05). The ROS level showed 1.3-fold increase (p < 0.05) at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.
Keywords: chalcone; synthetic; cytotoxicity; MCF-7 cells; apoptosis; high content screening; caspase; ROS chalcone; synthetic; cytotoxicity; MCF-7 cells; apoptosis; high content screening; caspase; ROS
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Syam, S.; Abdelwahab, S.I.; Al-Mamary, M.A.; Mohan, S. Synthesis of Chalcones with Anticancer Activities. Molecules 2012, 17, 6179-6195.

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