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      Synthesis of Chalcones with Anticancer Activities

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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 IC 50 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.

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          Most cited references32

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            Natural products as leads to anticancer drugs.

            Throughout history, natural products have afforded a rich source of compounds that have found many applications in the fields of medicine, pharmacy and biology. Within the sphere of cancer, a number of important new commercialised drugs have been obtained from natural sources, by structural modification of natural compounds, or by the synthesis of new compounds, designed following a natural compound as model. The search for improved cytotoxic agents continues to be an important line in the discovery of modern anticancer drugs. The huge structural diversity of natural compounds and their bioactivity potential have meant that several products isolated from plants, marine flora and microorganisms can serve as "lead" compounds for improvement of their therapeutic potential by molecular modification. Additionally, semisynthesis processes of new compounds, obtained by molecular modification of the functional groups of lead compounds, are able to generate structural analogues with greater pharmacological activity and with fewer side effects. These processes, complemented with high-throughput screening protocols, combinatorial chemistry, computational chemistry and bioinformatics are able to afford compounds that are far more efficient than those currently used in clinical practice. Combinatorial biosynthesis is also applied for the modification of natural microbial products. Likewise, advances in genomics and the advent of biotechnology have improved both the discovery and production of new natural compounds.
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              A review of anti-infective and anti-inflammatory chalcones.

              Chalcones, considered as the precursors of flavonoids and isoflavonoids, are abundant in edible plants, and have also been shown to display a diverse array of pharmacological activities. The purpose of this review is to provide an overview of the pharmacological activity of synthetic and naturally occurring chalcones. This review is complementary to earlier reviews and covers more recent reports of antimicrobial activity of chalcones (antibacterial and antifungal), as well as antileishmanial, antimalarial, antiviral and anti-inflammatory activities of these compounds.
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                Author and article information

                Journal
                Molecules
                Molecules
                molecules
                Molecules
                MDPI
                1420-3049
                25 May 2012
                June 2012
                : 17
                : 6
                : 6179-6195
                Affiliations
                [1 ]UPM-MAKNA Cancer Research Lab, Institute of Bioscience, University Putra Malaysia, 43400 Serdang, Selangor, Malaysia; Email: suvithaavs@ 123456gmail.com
                [2 ]Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia; Email: siddigroa@ 123456yahoo.com
                [3 ]Department of Chemistry, Faculty of Science and Arts in Al-Mukhwah, Al-Baha University, Al-Baha 65431, Saudi Arabia; Email: almamarym@ 123456hotmail.com
                [4 ]Centre for Natural Products and Drug Discovery (CENAR), Department of Pharmacology, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia; Email: syammohanm@ 123456yahoo.com
                Author notes
                [* ] Author to whom correspondence should be addressed; Email: siddigroa@ 123456yahoo.com ; Tel.: +603-7967-4909; Fax: +603-7967-4964.
                Article
                molecules-17-06179
                10.3390/molecules17066179
                6268294
                22634834
                50fd6493-1407-423f-a5a6-4faac05c293a
                © 2012 by the authors; licensee MDPI, Basel, Switzerland.

                This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                : 28 March 2012
                : 20 April 2012
                : 27 April 2012
                Categories
                Article

                cytotoxicity,chalcone,synthetic,mcf-7 cells,apoptosis,high content screening,caspase,ros

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