One-pot synthesis of cinnamylideneacetophenones and their in vitro cytotoxicity in breast cancer cells |
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| Institution: | 1. Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States;2. Department of Pharmaceutical Sciences, Hampton University, Hampton, VA, United States;3. Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States;4. Department of Chemistry, Geology and Physics, School of Mathematics, Science & Technology, Elizabeth City State University, Elizabeth City, NC, United States;5. Department of Neuroscience and Pharmacology, Meharry Medical College, Nashville, TN, United States;6. Department of Chemistry, University of California, Riverside, CA 92521, United States;1. Department of Physics, Madras Christian College, Chennai, 600059, Tamilnadu, India;2. University of Madras, Chennai, 600005, Tamilnadu, India;3. Department of Physics, Arignar Anna Govt. Arts College, Cheyyar, 604407, Tamilnadu, India;1. Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, No. 152, Luoyu Road, Hongshan District, Wuhan 430079, PR China;2. Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research, Jiangsu Simcere Pharmaceutical Co. Ltd, Nanjing 210042, PR China;3. State Key Laboratory of Agricultural Microbiology, College of Plant Science and Technology, Huazhong Agricultural University, Wuhan 430070, PR China;1. Graduate School of Pharmaceutical Sciences, Osaka University, Yamada-oka 1-6, Suita, Osaka 565-0871, Japan;2. Department of Molecular-Targeting Cancer Prevention, Kyoto Prefectural University of Medicine, Kawaramachi-Hirokoji, Kamigyo-ku, Kyoto 602-8566, Japan;1. Department of Integrative Biology and Physiology, Department of Chemistry and Biochemistry, and Institute of Quantiative and Computational Biology, University of California - Los Angeles, Los Angeles, California;1. Drug Design & Discovery Laboratory, Department of Pharmaceutical Sciences, Sam Higginbottom Institute of Agriculture, Technology & Sciences, Formerly Allahabad Agricultural Institute, Deemed University, Allahabad 211007, India;2. Anand College of Pharmacy, Agra 282007, India |
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| Abstract: | A series of cinnamylideneacetophenones were synthesized via a modified Claisen–Schmidt condensation reaction and evaluated for cytotoxicity against breast cancer cells using the Alamar Blue™ assay. Derivatives 17 and 18 bearing a 2-nitro group on the B ring, exhibited sub-micromolar cytotoxicity in MCF-7 cells (IC50 = 71 and 1.9 nM), respectively. Derivative 17 also displayed sub-micromolar (IC50 = 780 nM) cytotoxicity in MDA-MB-468 cells. Additionally, 17 and 18 displayed significantly less cytotoxicity than the chemotherapeutic doxorubicin in non-tumorigenic MCF-10A cells. This study provides evidence supporting the continued development of nitro-substituted cinnamylideneacetophenones as small molecules to treat breast cancer. |
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| Keywords: | Breast cancer Estrogen receptor Chalcone derivatives Leinamycin Cytotoxicity |
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