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Bioactive atropisomers: Unraveling design strategies and synthetic routes for drug discovery.
Liu, Shuai-Jiang; Zhao, Qian; Liu, Xiao-Chen; Gamble, Allan B; Huang, Wei; Yang, Qian-Qian; Han, Bo.
Afiliação
  • Liu SJ; State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, School of Basic Medical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • Zhao Q; School of Pharmacy, University of Otago, Dunedin, New Zealand.
  • Liu XC; State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, School of Basic Medical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • Gamble AB; State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, School of Basic Medical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • Huang W; School of Pharmacy, University of Otago, Dunedin, New Zealand.
  • Yang QQ; State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, School of Basic Medical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • Han B; State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, School of Basic Medical Sciences, Chengdu University of Traditional Chinese Medicine, Chengdu, China.
Med Res Rev ; 44(5): 1971-2014, 2024 09.
Article em En | MEDLINE | ID: mdl-38515232
ABSTRACT
Atropisomerism, an expression of axial chirality caused by limited bond rotation, is a prominent aspect within the field of medicinal chemistry. It has been shown that atropisomers of a wide range of compounds, including established FDA-approved drugs and experimental molecules, display markedly different biological activities. The time-dependent reversal of chirality in atropisomers poses complexity and obstacles in the process of drug discovery and development. Nonetheless, recent progress in understanding atropisomerism and enhanced characterization methods have greatly assisted medicinal chemists in the effective development of atropisomeric drug molecules. This article provides a comprehensive review of their special design thoughts, synthetic routes, and biological activities, serving as a reference for the synthesis and biological evaluation of bioactive atropisomers in the future.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Descoberta de Drogas Limite: Animals / Humans Idioma: En Revista: Med Res Rev Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Descoberta de Drogas Limite: Animals / Humans Idioma: En Revista: Med Res Rev Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China