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)

Title

Heterocyclic Communications

Publisher

De Gruyter

Publisher Country

Germany

Indexing

Thomson Reuters

Impact Factor

1.057

Publication Type

Both (Printed and Online)

Volume

26

Year

2020

Pages

157–167