Heterocyclic communications | |
Synthesis and Biological Evaluation of Benzodioxole Derivatives as Potential Anticancer and Antioxidant agents | |
article | |
Mohammed Hawash1  Tahrir Shtayeh1  Hadeel Sawaftah1  Ahmed Mousa2  Ahmad M Eid1  Nidal Jaradat1  Murad Abualhasan1  Johnny Amer2  Abdel Naser Zaid1  Saja Draghmeh1  Donia Daraghmeh1  Haifa Daraghmeh1  | |
[1] Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University;Department of Biomedical Sciences, Pharmacology & Toxicology Division. Faculty of Medicine and Health Sciences, An-Najah National University | |
关键词: Benzodioxole; Anticancer; Antioxidant; Doxorubicin; Trolox; | |
DOI : 10.1515/hc-2020-0105 | |
学科分类:内科医学 | |
来源: De Gruyter | |
【 摘 要 】
a series of benzodioxole compounds were synthesized and evaluated for their cytotoxic activity against cervical (Hela), colorectal (Caco-2), and liver (Hep3B) cancer cell lines. Compounds 5a, 5b, 6a, 6b, 7a and 7b showed very weak or negligible anticancer activity with IC 50 3.94-9.12 mM. On the contrary, carboxamide containing compounds 2a and 2b showed anticancer activity. Both 2a and 2b reduced Hep3B secretions of α-fetoprotein (α-FP) to 1625.8 ng/ml and 2340 ng/ml, respectively, compared to 2519.17 ng/ml in untreated cells. The results also showed that compound 2a has potent anticancer activity against Hep3B cancer cell line. Furthermore, in cell cycle analysis, compound 2a induced arrest in the G2-M phase in value of 8.07% that was very close to the activity of doxorubicin (7.4%). These results indicate that compound 2a has a potent and promising antitumor activity. However, benzodiazepine derivatives ( 7a and 7b) showed moderate antioxidant activity with IC 50 values of 39.85 and 79.95 μM, respectively compared with the potent antioxidant agent Trolox (IC 50 = 7.72 μM).
【 授权许可】
CC BY|CC BY-NC-ND
【 预 览 】
Files | Size | Format | View |
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RO202107200002206ZK.pdf | 294KB | download |