Background: Colorectal cancer is the third most common form of cancer in both men and women
around the world. The chemistry and biological study of heterocyclic compounds have been an interesting area
for a long time in pharmaceutical and medicinal chemistry.
Methods: A new synthetic compound, 2-(1,1-dimethyl-1H-benzo[e]indol-2-yl)-3-((2-hydroxyphenyl)amino)
acrylaldehyde, abbreviated as DBID, was prepared through the reaction of 2-(diformylmethylidene)-1,1-
dimethylbenzo[e]indole with 2-aminophenol. The chemical structure of the synthesized compound was characterized
by 1H NMR, 13C NMR and APT-NMR spectroscopy and confirmed by elemental analysis (CHN). The compound
was screened for the antiproliferation effect against colorectal cancer cell line, HCT 116 and its possible
mechanism of action was elucidated. To determine the IC50 value, the MTT assay was used and its apoptosisinducing
effect was investigated.
Results: DBID inhibited the proliferation of HCT 116 cells with an IC50 of 9.32 µg/ml and significantly increased the
levels of caspase -8, -9 and -3/7 in the treated cells compared to untreated cells. Apoptosis features in HCT 116 cell
was detected in treated cells by using the AO/PI staining that confirmed that the cells had undergone remarkable
morphological changes in apoptotic bodies. Furthermore, this changes in expression of caspase -8, -9 and -3 were
confirmed by gene and protein quantification using RT-PCR and western blot analysis, respectively.
Conclusion: The current study showed that the DBID compound has demonstrated chemotherapeutic activity which
was evidenced by significant increases in the expression and activation of caspase and exploit the apoptotic signaling
pathways to trigger cancer cell death.