A Facile Ugi/Ullmann Cascade Reaction to Access Fused Indazolo-Quinoxaline Derivatives with Potent Anticancer Activity
Yong Li,
Liujun He,
Hongxia Qin,
Yao Liu,
Binxin Yang,
Zhigang Xu,
Donglin Yang
Affiliations
Yong Li
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
Liujun He
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
Hongxia Qin
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
Yao Liu
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
Binxin Yang
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
Zhigang Xu
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
Donglin Yang
College of Pharmacy, National & Local Joint Engineering Research Center of Targeted and Innovative Therapeutics, Chongqing University of Arts and Sciences, Chongqing 402160, China
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 6e inhibits human colon cancer cell HCT116 proliferation with an IC50 of 2.1 μM, suggesting potential applications for developing a drug lead in medicinal chemistry.
