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

Heterocyclic communications

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