Synthesis and Biological Evaluation of Benzodioxole Derivatives as Potential Anticancer and Antioxidant agents

Heterocyclic Communications

Mousa Ahmed¹  Amer Johnny¹  Abualhasan Murad²  Shtayeh Tahrir²  Hawash Mohammed²  Jaradat Nidal²  Daraghmeh Haifa²  Eid Ahmad M²  Draghmeh Saja²  Daraghmeh Donia²  Sawaftah Hadeel²  Naser Zaid Abdel² 

[1] Department of Biomedical Sciences, Physiology, Pharmacology & Toxicology Division. Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine;Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, NablusP.O. Box 7, 00970, Palestine;

关键词: benzodioxole;    anticancer;    antioxidant;    doxorubicin;    trolox;   

DOI  :  10.1515/hc-2020-0105

来源: DOAJ

【 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 IC50 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 IC50 values of 39.85 and 79.95 μM, respectively compared with the potent antioxidant agent Trolox (IC50 = 7.72 μM).

【 授权许可】

Unknown