In vitro cytotoxicity evaluation of thiourea derivatives bearing Salix sp. constituent against HK-1 cell lines
In searching for drugs from natural product scaffolds has gained interest among researchers. In this study, a series of twelve halogenated thiourea (ATX 1-12) via chemical modification of aspirin (a natural product derivative) and evaluated for cytotoxic activity against nasopharyngeal carcinoma...
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| 主要な著者: | , , , |
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| フォーマット: | 論文 |
| 言語: | English |
| 出版事項: |
2018
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| 主題: | |
| オンライン･アクセス: | http://eprints.unisza.edu.my/6141/1/FH02-FF-18-19751.pdf http://eprints.unisza.edu.my/6141/ |
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| 要約: | In searching for drugs from natural product scaffolds has gained interest
among researchers. In this study, a series of twelve halogenated
thiourea (ATX 1-12) via chemical modification of aspirin (a natural
product derivative) and evaluated for cytotoxic activity against nasopharyngeal
carcinoma (NPC) cell lines, HK-1 via MTS-based colorimetric
assay. The cytotoxicity studies demonstrated that halogens at meta position
of ATX showed promising activity against HK-1 cells (IC50 value
�15 mM) in comparison to cisplatin, a positive cytotoxic drug (IC50 value
¼8.9±1.9 mM). ATX 11, bearing iodine at meta position, showed robust
cytotoxicity against HK-1 cells with an IC50 value of 4.7±0.7mM.
Molecular docking interactions between ATX 11 and cyclooxygenase-2
demonstrated a robust binding affinity value of �8.1 kcal/mol as compared
to aspirin’s binding affinity value of �6.4 kcal/mol. The findings
represent a promising lead molecule from natural product with excellent
cytotoxic activity against NPC cell lines. |
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