A facile one-pot method for the synthesis of new phenanthrene fused-dihydrodibenzo-quinolinone derivatives has been successfully accomplished by employing sulfamic acid as catalyst. These new compounds were evaluated for their in vitro cytotoxic potential against human lung (A549), prostate (PC-3 and DU145), breast (MCF-7) and colon (HT-29 and HCT-116) cancer cell lines. Among all the tested compounds, one of the derivatives 8p showed good anti-proliferative activity against A549 lung cancer cell line with an IC₅₀ of 3.17 ± 0.52 µM. Flow cytometric analyses revealed that compound 8p arrested both Sub G1 and G2/M phases of cell cycle in a dose dependent manner. The compound 8p also displayed significant inhibition of tubulin polymerization and disruption of microtubule network (IC₅₀ of 5.15 ± 0.15 µM). Molecular docking studies revealed that compound 8p efficiently interacted with critical amino acid Cys241 of the α/β-tubulin by a hydrogen bond (SH…O = 2.4 Å). Further, the effect of 8p on cell viability was also studied by AO/EB, DCFDA and DAPI staining. The apoptotic characteristic features revealed that 8p inhibited cell proliferation effectively through apoptosis by inducing the ROS generation. Analysis of mitochondrial membrane potential through JC-1 staining and annexin V binding assay indicated the extent of apoptosis in A549 cancer cells.

通过使用氨基磺酸作为催化剂，已经成功地完成了一种简便的一锅法合成新的菲稠二苯并二氢二苯并喹啉酮衍生物的方法。评估了这些新化合物对人肺（A549），前列腺（PC-3和DU145），乳腺癌（MCF-7）和结肠（HT-29和HCT-116）癌细胞的体外细胞毒性潜力。在所有测试化合物中，一种衍生物8p对A549肺癌细胞系表现出良好的抗增殖活性，IC ₅₀为3.17±0.52 µM。流式细胞仪分析显示化合物8p以剂量依赖的方式阻止了细胞周期的Sub G1和G2 / M期。复合8p还显示出对微管蛋白聚合的显着抑制和微管网络的破坏（IC ₅₀为5.15±0.15 µM）。分子对接研究表明，化合物8p通过氢键与α/β-微管蛋白的关键氨基酸Cys241有效相互作用（S H…O = 2.4Å）。此外，还通过AO / EB，DCFDA和DAPI染色研究了8p对细胞活力的影响。凋亡的特征表明，8p通过诱导ROS的产生，通过凋亡有效地抑制了细胞的增殖。通过JC-1染色和膜联蛋白V结合试验分析线粒体膜电位，表明A549癌细胞的凋亡程度。