Background: Compounds containing furo[3,2-b]pyridine framework have shown interesting pharmacological properties, including anticancer activities. Though these compounds are generally synthesized via the heteroannulation processes involving acetylenic derivatives, some of them are complex.

Objective: The study aimed to explore a series of 2-substituted furo[3,2-b]pyridines for their cytotoxic properties against cancer cell lines in vitro.

Methods: We developed a convenient synthesis of 2-substituted furo[3,2-b]pyridines via sequential (i) C-C coupling followed by (ii) C-O bond-forming reactions in a single pot. The reactions were performed under ultrasound irradiation in the presence of Pd/C as an inexpensive, stable and widely used catalyst. A range of 2- substituted furo[3,2-b]pyridines were synthesized via coupling of 3-chloro-2-hydroxy pyridine with terminal alkynes in the presence of 10% Pd/C-CuI-PPh3-Et3N in EtOH. The in vitro evaluation of all these compounds was carried out against MDA-MB-231 and MCF-7 cell lines and subsequently against SIRT1.

Results: The furo[3,2-b]pyridine derivative 3b showed encouraging growth inhibition of both MDAMB-231 and MCF-7 cell lines and inhibition of SIRT1. The compound 3b also showed apoptosis-inducing potential when tested against MCF-7 cells.

Conclusion: The Pd/C-Cu catalysis under ultrasound accomplished a one-pot and direct access to 2-substituted furo[3,2-b]pyridine derivatives, some of which showed anticancer properties.

背景：含有呋喃并[3,2-b]吡啶骨架的化合物已显示出令人感兴趣的药理特性，包括抗癌活性。尽管这些化合物通常是通过涉及炔属衍生物的杂环化过程合成的，但其中一些化合物很复杂。

目的：该研究旨在探索一系列2-取代的呋喃并[3,2-b]吡啶类化合物，它们在体外对癌细胞系具有细胞毒性。

方法：我们通过顺序（i）CC偶联，然后（ii）在一个罐中形成CO键的反应，开发了一种方便的2取代的呋喃并[3,2-b]吡啶的合成方法。反应是在Pd / C存在下作为廉价，稳定和广泛使用的催化剂在超声辐射下进行的。在10％Pd / C-CuI-PPh3-Et3N在EtOH中的存在下，通过将3-氯-2-羟基吡啶与末端炔烃偶联，合成了一系列2-取代的呋喃并[3,2-b]吡啶。针对MDA-MB-231和MCF-7细胞系，然后针对SIRT1，对所有这些化合物进行了体外评估。

结果：呋喃并[3,2-b]吡啶衍生物3b对MDAMB-231和MCF-7细胞系均显示出令人鼓舞的生长抑制作用，并对SIRT1产生抑制作用。当针对MCF-7细胞进行测试时，化合物3b还显示出诱导凋亡的潜力。

结论：超声作用下的Pd / C-Cu催化反应可实现一锅直接接触2-取代的呋喃[3,2-b]吡啶衍生物，其中一些具有抗癌作用。