The design and synthesis of substituted 1-(1-ethy-1H-benzimidazol-2-yl) ethanone (3a-f) and substituted 1-(2-bromoethyl)-2-
(1-hydrazinylidene or ethylidene)-1H-benzimidazole (3g-j) have been successfully achieved under microwave irradiation with an aim for
finding promising anticancer agents. Among the synthetic compounds, those with potential activity were selected and evaluated in-vitro
for anticancer activity at the National Cancer Institute (NCI), USA, against 60 cancer cell lines from nine types of human cancer. The title
compound 3e (NSC: 765733/1) exhibited notable growth inhibition that satisfies threshold criteria at single dose (10 µM) on all human
cell lines of NCI. This compound was considered for further study at five dose levels (0.01, 0.1, 1, 10 and 100 µM) with GI50 values
ranging from 0.19 to 92.7 µM. Compound 3e was found superior for Non-small cell lung cancer cell lines (HOP-92) and calculated end
points (GI50 0.19, TGI 1.45, LC50 >100 and Log10GI50 -6.70, Log10TGI -5.84, Log10LC50 >-4.00). Docking study was performed using
Maestro 9.0 to provide binding mode into binding sites of topoisomerase enzyme (PDB ID: 1SC7). Hopefully in the future, compound 3e
could be used as novel template for the development of potential anticancer agents.
Keywords: Anticancer compounds, bendamustine, benzimidazole, chlorambucil, NCI-60 human cell lines, sulforhodamine B.
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