Background: Privileged 4H-chromenes possess potent anticancer and anticonvulsant
activities. By the inspiring potency of 4H-chromenes and demands of the present era of scaffolds,
an effective molecule was discovered for the treatment of cancer and related diseases.
Objective: This study designed and synthesized a novel series of 4H-chromene derivatives from
one-port synthesis for the treatment of cancer and other such diseases.
Methods: A side amide chain was substituted in multiple steps on the amine group of chromene.
Later, the anticancer activity of synthesized compounds was investigated against the human colon
adenocarcinoma cell line (HT-29) using sulforhodamine B (SRB) assay. Moreover, anticonvulsant
activity was also detected using maximal electroshock seizure (MES) model and subcutaneous
Metrazol Seizure Threshold Test (scMET) in albino Wistar rats. Neurotoxicity was evaluated by
using the rotarod test. Before the synthesis, docking studies were performed using various molecular
targets. Subsequently, the computational study of the titled compounds was performed to predict
the pharmacokinetic profile.
Results: Among the fifteen tested compounds, A4 and A9 were found to be active against HT-29
cells (growth inhibitory dose 50% (GI50) <11μM). Moreover, compounds A4 showed the protection
at 300mg/kg in scMET (h) for albino Wistar rats and compounds A9, A11, and A15 exhibited
the anticonvulsant effect at the doses 100, 300 and 300 mg/kg, respectively in MES screen (h).
Conclusion: Due to these encouraging results, we concluded that both A4 and A9 may be effective
for treatement against colon cancer, while compound A9 may be used as a considerable effective
molecule for the treatment of epilepsy.