Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton

Kangjia Sheng (1, 2) , Yiming Song (1) , Fan Lei (1) , Wanqing Zhao (1) , Liming Fan (1) , Lei Wu (1) , Yubo Liu (1) , Shaoping Wu (1) , Yongmin Zhang (1, 3)

1 Northwest University (Xi'an)
2 Xjtu - Xi'an Jiaotong University
3 IPCM - Institut Parisien de Chimie Moléculaire

The tetralone and tetralone derivatives, as crucial structural scaffolds of potential novel drugs targeted at multiple biological end-points, are normally found in several natural compounds and also, it can be used as parental scaffold and/or intermediate for the synthesis of a series of pharmacologically active compounds with a broad-spectrum of bioactivities including antibacterial, antitumor, CNS effect and so on. Meanwhile, SAR information of its analogues has drawn attentions among medicinal chemists, which could contribute to the further research related to tetralone derivatives aimed at multiple targets. This review encompasses pharmacological activities, SAR analysis and docking study of tetralone and its derivatives, expecting to provide a general retrospect and prospect on tetralone derivatives.

Mots clés: Tetralone; tetralone derivatives; antibacterial; antitumor; CNS effect; SAR

Domaines: Biochimie, Biologie Moléculaire

Kangjia Sheng, Yiming Song, Fan Lei, Wanqing Zhao, Liming Fan, et al.. Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. European Journal of Medicinal Chemistry, 2022, 227, pp.113964. ⟨10.1016/j.ejmech.2021.113964⟩. ⟨hal-03414368⟩