Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines |
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| Affiliation: | 1. Department of Plant Science, Plant Sciences Complex, University of Pretoria, Pretoria 0002, South Africa;2. Department of Natural Products, National Institute of Pharmaceutical Education and Research, Ahmedabad 380054, India;3. Department of Biochemistry and Microbiology, Nelson Mandela Metropolitan University, Summerstrand Campus, Port Elizabeth 6031, South Africa;4. Pharmaceutical Sciences Division, King’s College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NN, UK;1. School of Chemical Engineering, Yeungnam University, Gyeongsan 712-749, Republic of Korea;2. Department of Food Science and Technology, Yeungnam University, Gyeongsan 712-749, Republic of Korea;3. Analysis Research Division, Daegu Center, Korea Basic Science Institute, Daegu 702-701, Republic of Korea;1. Departamento de Química Orgánica, Facultad de Química, Pontificia Universidad Católica de Chile, 702843 Santiago de Chile, Chile;2. Centro Singular de Investigación en Química Biológica y Materiales Moleculares and Departamento de Química Orgánica (Facultad de Química), Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain;3. Facultad de Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N 1093, Valparaíso, Chile;4. Centro de Investigaciones Biomédicas, Escuela de Medicina, Universidad de Valparaíso, Av. Hontaneda N° 2664, Valparaíso, Chile;5. Instituto de Ciencias Biomédicas, Programa de Farmacología Molecular y Clínica, Universidad de Chile, PO Box 70000, Santiago, Chile;6. Departamento de Química, Facultad de Ciencias, Universidad de Chile, PO Box 653, Santiago, Chile;1. FSTox Consulting Ltd., Raunds, UK;2. BASF SE, Ludwigshafen, Germany;3. Kirkland Consulting, Tadcaster, UK;1. Servicio de Estudios, Documentación y Estadística, Consejería de Sanidad de la Junta de Castilla y León, Valladolid, Spain;2. Dirección Médica, Hospital Clínico Universitario de Valladolid, Valladolid, Spain;3. Gerencia de Atención Primaria Valladolid-Oeste, Valladolid, Spain;4. Departamento de Microbiología, Facultad de Medicina, Universidad de Valladolid, Valladolid, Spain;1. Division of Pharmaceutical Chemistry, Faculty of Pharmacy, Rhodes University, Grahamstown, 6140, South Africa;2. Department of Biotechnology, Rhodes University, Grahamstown, 6140, South Africa;3. Department of Biochemistry and Microbiology, Rhodes University, Grahamstown, 6140, South Africa;4. Centre for Chemico- and Biomedicinal Research, Rhodes University, Grahamstown, 6140, South Africa;5. Drug Discovery and Development Centre (H3-D), Department of Chemistry, University of Cape Town, Rondebosch, 7701, South Africa;6. Molecular Mycobacteriology Research Unit, Department of Pathology and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town, South Africa;7. Department of Pharmacology, University of Pretoria, Pretoria, South Africa;8. Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa |
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| Abstract: | In an effort to establish new candidates with enhanced anticancer activity of 5-hydroxy-7-methyl-1,4-naphthoquinone scaffold (7-methyljuglone) previously isolated from the root extract of Euclea natalensis, a series of 7-methyljuglone derivatives have been synthesized and assessed for cytotoxicity on selected human cancer lines. These compounds were screened in vitro for anticancer activity on MCF-7, HeLa, SNO and DU145 human cancer cell lines by MTT assay. Most of them exhibited significant toxicity on cancer cell lines with lower IC50 values. The most potent derivative (19) exhibited the toxicity on HeLa and DU145 cell lines with IC50 value of 5.3 and 6.8 μM followed by compound (5) with IC50 value of 10.1 and 9.3 μM, respectively. Structure–activity relationship reveals that the fluoro substituents at position C-8 while hydroxyl substituents at C-2 and C-5 positions played an important role in toxicity. |
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| Keywords: | 7-Methyljuglone derivatives Cytotoxicity Cell cycle analysis Cell apoptosis |
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