A series of new β-carboline-bisindole compounds were designed, synthesized and evaluated for their antiproliferative activity against human cancer cell lines, such as A549 (lung cancer), DU-145 (prostate cancer), HeLa (cervical cancer) and MCF-7 (breast cancer). All the compounds exhibited considerable antiproliferative activity. Among them, compounds 7g and 7r exhibited significant antiproliferative activity against DU-145 cells with IC₅₀ values 1.86 and 1.80 μM respectively. Further, these compounds effectively inhibit DNA topoisomerase I activity and can also cleave the pBR322 plasmid upon irradiation with UV light. In addition, Annexin V-FITC assay suggested that these compounds induced apoptosis in DU- 145 cell line (prostate cancer). To know the binding mode of these compounds with DNA, spectroscopic studies were also carried out. These new compounds were showing a unique mode of binding with DNA, both biophysical studies such as UV–Visible, fluorescence, circular dichroism and molecular docking studies revealed that the β-carboline-bisindole compounds exhibit combilexin type of interaction with DNA.

设计，合成和评估了一系列新的β-咔啉-双吲哚化合物对人类癌细胞系（例如A549（肺癌），DU-145（前列腺癌），HeLa（宫颈癌）和MCF- 7（乳腺癌）。所有化合物均显示出相当大的抗增殖活性。其中，化合物7g和7r对具有IC _50的DU-145细胞表现出显着的抗增殖活性值分别为1.86和1.80μM。此外，这些化合物有效抑制DNA拓扑异构酶I活性，并且还可以在用紫外线照射时切割pBR322质粒。另外，膜联蛋白V-FITC测定表明这些化合物诱导DU-145细胞系（前列腺癌）中的细胞凋亡。为了了解这些化合物与DNA的结合方式，还进行了光谱研究。这些新化合物显示出与DNA结合的独特模式，无论是生物物理研究，例如紫外可见，荧光，圆二色性和分子对接研究，都表明β-咔啉-双吲哚化合物表现出与DNA相互作用的梳理类型。