Synthesis and SAR studies of bis-chromenone derivatives for anti-proliferative activity against human cancer cells |
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| Affiliation: | 1. College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea;2. Bio-Evaluation Center, KRIBB, Cheongwon-gun Chungcheongbuk-do 363-883, Republic of Korea;1. USDA-ARS Invasive Insect Biocontrol and Behavior Laboratory, B-007, BARC-West Beltsville, MD 20705, USA;2. Environmental Quality Laboratory, B-007, BARC-West Beltsville, MD 20705, USA;1. Physics Department, Faculty of Science and Arts, AlJouf University, Jouf, Saudi Arabia;2. Thin Film Laboratory, Physics Department, Faculty of Education, Ain Shams University, Roxy 11711, Cairo, Egypt;3. Electronics Materials Dep. Advanced Technology & New Materials Research Inst., City of Scientific Research & Technological Applications (SRTA-City), New Borg El-Arab City, P.O. Box: 21934, Alexandria, Egypt;4. Department of Chemistry, Faculty of Education, Ain Shams University, Roxy 11711, Cairo, Egypt;1. Molecular Synthesis and Drug Discovery Laboratory, Center of Biomedical Research, Sanjay Gandhi Post-Graduate Institute of Medical Sciences Campus, Raebareli Road, Lucknow, 226014, India;2. Division of Organic Synthesis and Process Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500007, India;3. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India;1. School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, 920-1192, Japan;2. Graduate School of Pharmacy, Meijo University, Tempaku-ku, Nagoya, 468-8503, Japan;3. Molecular Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, Frederick, MD, 21702, United States;4. Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC, 27599-7568, United States |
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| Abstract: | A novel family of 3-((4-oxo-4H-chromen-3-yl)methyl)-4H-chromen-4-one (bis-chromone) derivatives were designed, synthesized and studied for their anti-cancer activity using the XTT assay for the growth inhibition against various human cancer cells. Among them, 3-((5-(cyclohexylmethoxy)-4-oxo-4H-chromen-3-yl)methyl)-7-methoxy-4H-chromen-4-one and 3-((5-(cyclohexylmethoxy)-4-oxo-4H-chromen-3-yl)methyl)-7-hydroxy-4H-chromen-4-one showed micromolar level of in vitro anti-proliferative activity against human cancer cell lines. The SAR studies indicated bis-chromone as a basic scaffold to design anticancer agents. The 5-cyclohexylmethoxy on the first chromenone ring and electron donating group such as CH3, OCH3 or hydrogen bonding group (OH) on the other chromenone ring of bis-chromone increased the activity. However, saturation of one of chromenone to chromanone in bis-chromones decreased the activity. |
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| Keywords: | Bis-chromone Anti-cancer Cytotoxicity |
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