In this work, five new hybrids of phenylsulfonylfuroxan merging 3-benzyl coumarin and their seco-B-ring derivatives 2–6 were designed and synthesized. Among them, compound 3 showed the most potent antiproliferation activities with IC₅₀ values range from 0.5 to 143 nM against nine drug-sensitive and four drug-resistant cancer cell lines. Preliminary pharmacologic studies showed that these compounds displayed lower toxicities than that of lead compound 1. Compound 3 obviously induced the early apoptosis and hardly affected the cell cycle of A2780, which was significantly different from compound 1. Especially, it gave 559- and 294-fold selectivity antiproliferation activity in P-gp overexpressed drug-resistant cancer cell lines MCF-7/ADR and KB-V compared to their drug-sensitive ones MCF-7 and KB, implying that compounds 2–6 might have an extra mechanism of anti-MDR-cancer with P-gp overexpression.

中文翻译：

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新型的一氧化氮的苯磺酰基呋喃喃和3-苄香豆素衍生物作为有效的抗肿瘤药。

在这项工作中，phenylsulfonylfuroxan合并3-苄基香豆素的五个新的杂种及其开环- B-环衍生物2 - 6设计并合成。其中，化合物3对9种药敏和4种耐药的癌细胞系表现出最强的抗增殖活性，IC ₅₀值在0.5至143 nM之间。初步的药理研究表明，这些化合物的毒性比铅化合物1低。化合物3明显诱导A2780的早期凋亡，几乎不影响A2780的细胞周期，这与化合物1有显着差异。。尤其是，与对药物敏感的MCF-7和KB相比，在过表达P-gp的耐药癌细胞系MCF-7 / ADR和KB-V中，它具有559倍和294倍的选择性抗增殖活性，这表明化合物2 – 6可能具有P-gp过表达的抗MDR癌症的额外机制。