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.

背景：特权4H-色烯具有有效的抗癌和抗惊厥活性。通过激发4H-色烯的潜力以及当今支架时代的需求，发现了一种有效的分子，可用于治疗癌症和相关疾病。

目的：本研究从单端口合成设计和合成了一系列新的4H-色烯衍生物，用于治疗癌症和其他此类疾病。

方法：将侧酰胺链分多个步骤取代在色烯的胺基上。随后，使用磺基罗丹明B（SRB）分析研究了合成化合物对人结肠腺癌细胞系（HT-29）的抗癌活性。此外，还使用最大的电击癫痫发作（MES）模型和皮下Metrazol癫痫发作阈值测试（scMET）在白化Wistar大鼠中检测到了抗惊厥活性。神经毒性通过旋转试验进行评估。在合成之前，使用各种分子靶进行了对接研究。随后，对标题化合物进行了计算研究，以预测药代动力学特征。

结果：在15种测试化合物中，发现A4和A9对HT-29细胞具有活性（生长抑制剂量50％（GI50）<11μM）。此外，化合物A4在scMET（h）中以300mg / kg的剂量显示对白化Wistar大鼠具有保护作用，化合物A9，A11和A15在MES筛选中分别以100、300和300 mg / kg的剂量显示出抗惊厥作用（h ）。

结论：由于这些令人鼓舞的结果，我们得出结论，A4和A9均可有效治疗结肠癌，而化合物A9可用作治疗癫痫的相当有效的分子。