Cytotoxicity of synthesized 1,4-naphthoquinone analogues on selected human cancer cell lines
| Autor: | Gerhardt J. Boukes, J.J. Marion Meyer, Namrita Lall, Navneet Kishore, Peter J. Houghton, Anita Mahapatra, Brigitte Binneman, Maryna van de Venter, Debbie du Plessis-Stoman |
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| Rok vydání: | 2014 |
| Předmět: |
Stereochemistry
Clinical Biochemistry ved/biology.organism_classification_rank.species Pharmaceutical Science Antineoplastic Agents 1 4-Naphthoquinone Euclea natalensis Biochemistry HeLa Structure-Activity Relationship chemistry.chemical_compound DU145 Drug Discovery Tumor Cells Cultured Humans MTT assay Cytotoxicity Molecular Biology Cell Proliferation Dose-Response Relationship Drug Molecular Structure biology Chemistry ved/biology Cell Cycle Organic Chemistry U937 Cells biology.organism_classification Apoptosis Cell culture MCF-7 Cells Molecular Medicine Drug Screening Assays Antitumor HeLa Cells Naphthoquinones |
| Zdroj: | Bioorganic & Medicinal Chemistry. 22:5013-5019 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2014.06.013 |
| Popis: | 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 6.8μM followed by compound (5) with IC50 value of 10.1 and 9.3μM, 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. |
| Databáze: | OpenAIRE |
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