Eleven novel acridone derivatives were synthesized and evaluated for their anticancer activity against 60 human cancer cell lines. Five compounds 8b, 8d, 8g, 8h, and 8k displayed very good in vitro antiproliferative activities well over 95% of the panels. The most active compound is 8k (5, 7-dibromo-3-phenyl-3,4-dihydroacridin-1 (2H)-one). In addition, 8k was the most sensitive agent in all 9 panels starting with prostate (0.075 µm), leukemia (0.116 µm), non-small cell lung cancer (0.164 µm), colon cancer (0.193 µm), CNS cancer (0.264 µm), melanoma (0.317 µm), renal cancer (0.403 µm), ovarian cancer (0.410 µm), and breast cancer (0.608 µm). Virtual screening studies also revealed that nine of the eleven compounds formed good binding interaction with the active site ATPase domain of human topoisomerase IIα (PDB: 1zxm). All nine derivatives exhibited binding affinities that ranged in values from −8.5 to −7.9 kcal/mol, indicating that they could be catalytic inhibitors of the nuclear enzyme, topoisomerase.

合成了十一种新的a啶酮衍生物，并评估了它们对60种人类癌细胞系的抗癌活性。五个化合物8b，8d，8g，8h和8k表现出非常好的体外抗增殖活性，远超过95％的样本。活性最高的化合物是8k（5，7-二溴-3-苯基-3,4-二氢ac啶-1（2H）-one）。另外8k在从前列腺（0.075 µm），白血病（0.116 µm），非小细胞肺癌（0.164 µm），结肠癌（0.193 µm），中枢神经系统癌（0.264 µm），黑素瘤（ 0.317 µm），肾癌（0.403 µm），卵巢癌（0.410 µm）和乳腺癌（0.608 µm）。虚拟筛选研究还显示，这11种化合物中的9种与人拓扑异构酶IIα（PDB：1zxm）的活性位点ATPase结构域形成了良好的结合相互作用。所有九种衍生物均表现出在-8.5至-7.9 kcal / mol范围内的结合亲和力，表明它们可能是核酶拓扑异构酶的催化抑制剂。