2. Academic Validation
  3. Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton

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

  • Eur J Med Chem. 2022 Jan 5:227:113964. doi: 10.1016/j.ejmech.2021.113964.
Kangjia Sheng 1,  Yiming Song 2,  Fan Lei 3,  Wanqing Zhao 3,  Liming Fan 3,  Lei Wu 3,  Yubo Liu 3,  Shaoping Wu 4,  Yongmin Zhang 5
Affiliations

Affiliations

  • 1 School of Pharmacy, Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, 229 Taibai Road, Xi'an, Shaanxi, 710069, China; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an, Shaanxi, 710061, China.
  • 2 School of Chemical Engineering, Northwest University, 229 Taibai Road, Xi'an, Shaanxi, 710069, China.
  • 3 School of Pharmacy, Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, 229 Taibai Road, Xi'an, Shaanxi, 710069, China.
  • 4 School of Pharmacy, Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, 229 Taibai Road, Xi'an, Shaanxi, 710069, China. Electronic address: wushaoping@nwu.edu.cn.
  • 5 School of Pharmacy, Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Biomedicine Key Laboratory of Shaanxi Province, Northwest University, 229 Taibai Road, Xi'an, Shaanxi, 710069, China; Sorbonne Université, CNRS, Institut Parisien de Chimie Moléculaire, UMR 8232, 4 Place Jussieu, 75005, Paris, France.
PMID: 34743062 DOI: 10.1016/j.ejmech.2021.113964
Abstract

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.

Keywords

CNS effect; SAR; Tetralone; antibacterial; antitumor; tetralone derivatives.

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