In this study, a series of novel 7H-benzo [c] [1,3] dioxolo [4, 5-f] chromen-7-one derivatives were obtained by structural modification of the lead compounds with Fissitungfine B.

A total 15 compounds were designed, synthesized and evaluated as inhibitors of tumor. These target compounds have the novel chemical structures that named three six-membered rings including one lactone six-membered ring. In vitro assay, the results showed that the target compounds have a broad spectrum and strong of anti-tumor activity. Such as the target compound 4n to MCF-7 was IC₅₀ = 0.35 ± 0.01 μM, to A-549 was IC₅₀ = 0.37 ± 0.01 μM, to Hela was IC₅₀ = 0.56 ± 0.02 μM, to MDC-803 was IC₅₀ = 0.53 ± 0.02 μM and COLO-205 was IC₅₀ = 0.50 ± 0.02 μM in vitro. At the same time, in vivo anti-tumor activity assay results showed that the target compounds had a good inhibitory effect on tumor growth. Among them, the target compound 4n had the best anti-tumor activity, it could inhibit tumor growth well at a low dose. The target compound 4n could be used as a candidate drug for further research and development, in order to be used as early as application in the clinical treatment of tumors.

在这项研究中，通过用Fissitungfine B对先导化合物进行结构修饰，获得了一系列新颖的7 H-苯并[ c ] [1,3]二恶唑[ 4,5- f ] chromen-7-one衍生物。

共设计，合成和评估了15种化合物作为肿瘤抑制剂。这些目标化合物具有新颖的化学结构，命名为三个六元环，其中包括一个内酯六元环。在体外测定中，结果表明目标化合物具有广谱性和强的抗肿瘤活性。例如目标化合物4n的MCF-7为IC ₅₀  = 0.35±0.01μM，至A-549为IC ₅₀  = 0.37±0.01μM，至Hela为IC ₅₀  = 0.56±0.02μM，至MDC-803为IC ₅₀  = 0.53±0.02μM，而COLO-205在体外的IC ₅₀  = 0.50±0.02μM 。同时，体内抗肿瘤活性测定结果表明，目标化合物对肿瘤的生长具有良好的抑制作用。其中，目标化合物4n具有最佳的抗肿瘤活性，在低剂量时可以很好地抑制肿瘤的生长。目标化合物4n可用作进一步研究和开发的候选药物，以便尽早用于肿瘤的临床治疗中。