A Facile Ugi/Ullmann Cascade Reaction to Access Fused Indazolo-Quinoxaline Derivatives with Potent Anticancer Activity

oleh: Yong Li, Liujun He, Hongxia Qin, Yao Liu, Binxin Yang, Zhigang Xu, Donglin Yang

Format: Article
Diterbitkan: MDPI AG 2024-01-01

Deskripsi

A facile methodology for the construction of a complex heterocycle indazolo-fused quinoxalinone has been developed via an Ugi four-component reaction (U-4CR) followed by an intramolecular Ullmann reaction. The expeditious process features an operationally simple approach, time efficiency, and a broad substrate scope. Biological activity was evaluated and demonstrated that compound <b>6e</b> inhibits human colon cancer cell HCT116 proliferation with an IC<sub>50</sub> of 2.1 μM, suggesting potential applications for developing a drug lead in medicinal chemistry.