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Synthesis of Chalcones with Anticancer Activities
UPM-MAKNA Cancer Research Lab, Institute of Bioscience, University Putra Malaysia, 43400 Serdang, Selangor, Malaysia
Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia
Department of Chemistry, Faculty of Science and Arts in Al-Mukhwah, Al-Baha University, Al-Baha 65431, Saudi Arabia
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; in revised form: 20 April 2012 / Accepted: 27 April 2012 / Published: 25 May 2012
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
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MDPI and ACS Style
Syam, S.; Abdelwahab, S.I.; Al-Mamary, M.A.; Mohan, S. Synthesis of Chalcones with Anticancer Activities. Molecules 2012, 17, 6179-6195.
Syam S, Abdelwahab SI, Al-Mamary MA, Mohan S. Synthesis of Chalcones with Anticancer Activities. Molecules. 2012; 17(6):6179-6195.
Syam, Suvitha; Abdelwahab, Siddig Ibrahim; Al-Mamary, Mohammed Ali; Mohan, Syam. 2012. "Synthesis of Chalcones with Anticancer Activities." Molecules 17, no. 6: 6179-6195.