Synthesis and potential antineoplastic activity of dehydroabietylamine imidazole derivatives
| العنوان: | Synthesis and potential antineoplastic activity of dehydroabietylamine imidazole derivatives |
|---|---|
| المؤلفون: | Zhou Mengyi, Jiuzhou Shi, Xu Sun, Zhao Fengyi, Dong Jiang, Lu Wen, Cao Fuliang, Xu Li, Fan Su, Feng Lin |
| المصدر: | MedChemComm. 9:2091-2099 |
| بيانات النشر: | Royal Society of Chemistry (RSC), 2018. |
| سنة النشر: | 2018 |
| مصطلحات موضوعية: | 0301 basic medicine, Pharmacology, A549 cell, biology, 010405 organic chemistry, Chemistry, Organic Chemistry, Pharmaceutical Science, biology.organism_classification, 01 natural sciences, Biochemistry, In vitro, Umbilical vein, 0104 chemical sciences, HeLa, 03 medical and health sciences, 030104 developmental biology, Apoptosis, Drug Discovery, Toxicity, Molecular Medicine, MTT assay, IC50 |
| الوصف: | To seek more efficient and lower toxicity anticancer compounds, several imidazole combining dehydroabietylamine derivatives including organic salts (L(1)–L(2)) and amides (L(3)–L(5)) were synthesized. Their antineoplastic activity against HeLa (cervix), MCF-7 (breast), A549 (lung) and HepG2 (liver) cells and HUVECs (umbilical vein, normal cells) in vitro were evaluated by MTT assay. The results unequivocally showed that nearly all compounds had better antineoplastic activity and lower toxicity than dehydroabietylamine (L(0)). For MCF-7 cells, L(2) (0.75 μM) and L(5) (2.17 μM) had higher anti-MCF-7 activity than L(0) and DOX. For A549 cells, L(1) (1.85 μM) and L(2) (4.37 μM) had higher anti-A549 activity than L(0); in particular, the IC(50) value of L(1) was much lower than that of DOX. Among these investigated compounds, L(2) and L(5) had lower IC(50) values (0.75 μM and 2.17 μM) against MCF-7 cells and lower toxicity, which suggested that they may be potential future anticancer drugs. In addition, L(1) and L(2) could suppress cancer cell proliferation by inducing apoptosis. L(1)–L(5) could bind with DNA through intercalation. |
| تدمد: | 2040-2511 2040-2503 |
| DOI: | 10.1039/c8md00487k |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81d97189b06eadaf6bad6a9d65ec27a5 https://doi.org/10.1039/c8md00487k |
| Rights: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....81d97189b06eadaf6bad6a9d65ec27a5 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 20402511 20402503 |
|---|---|
| DOI: | 10.1039/c8md00487k |