A series of novel compounds carrying 1,2,4-triazole scaffold was synthesized and evaluated for their anticancer
activity against a panel of cancer cell lines using MTT assay. Compounds 8a, 8b, 8c, 8d, 10b, 10e,
and 10 g showed remarkable antiproliferative activity against the tested cell lines. Compounds 8a, 8b, 8c,
8d, 10b, 10e, and 10 g with the least IC50 values in MTT assay were tested against three known anticancer
targets including EGFR, BRAF and Tubulin. The results revealed that compounds 8c and 8d showed almost
same BRAF inhibitory activity and were discovered to be potent inhibitors of cancer cell proliferation and
were also observed to be strong Tubulin inhibitors. Moreover, 8c also showed the best EGFR inhibition
with IC50 = 3.6 lM. Finally molecular modeling studies were performed to explore the binding mode
of the most active compounds to the target enzymes.