Indole-based chalcones have been identified as interesting compounds with anticancer properties. In the present study, we report the synthesis and evaluation of new 1-methoxyindole and 2-alkoxyindole chalcone hybrids as antiproliferative agents active against colorectal carcinoma cell line. Among the 19 investigated molecules, four inhibit the proliferation of colorectal cancer cells HCT-116 with IC₅₀ values <8 µM and display low cytotoxicity to fibroblast cell line 3T3. The UV–visible, CD and fluorescence competitive displacement assays with ethidium bromide and Hoechst 33258 performed with two active chalcones demonstrated that investigated chalcones interact with calf thymus (CT) DNA through the groove binding mode. Likewise, the quenching interaction of chalcones with bovine serum albumin (BSA) was studied in vitro under optimal physiological condition (pH = 7.4). The Stern–Volmer constant for chalcone-BSA system was found in the range of 10⁵ M⁻¹.

吲哚基查耳酮已被鉴定为具有抗癌特性的有趣化合物。在本研究中，我们报告了新的1-甲氧基吲哚和2-烷氧基吲哚查尔酮杂种的合成和评估，这些杂种作为对大肠癌细胞系具有活性的抗增殖剂。在研究的19种分子中，有4种具有IC ₅₀抑制结直肠癌细胞HCT-116的增殖值<8 µM，对成纤维细胞3T3细胞毒性低。用溴化乙锭和Hoechst 33258进行的紫外线-可见，CD和荧光竞争性置换测定法是对两个活性查耳酮进行的，这表明所研究的查耳酮通过凹槽结合模式与小牛胸腺（CT）DNA相互作用。同样，在最佳生理条件（pH = 7.4）下，体外研究了查耳酮与牛血清白蛋白（BSA）的猝灭相互作用。查尔酮-BSA系统的斯特恩-沃尔默常数在10 ⁵  M ^-1范围内。