Journal
- MedComm Introduction
- Molecular Biomedicine Introduction
- Signal Transduction and Targeted Therapy Introduction
- MedComm | Incidence and risk factors of second primary cancer after the initial primary human papillomavirus related neoplasms
- Molecular Biomedicine | The bone marrow niche components are adversely affected in sepsis
Chief-in-Editor：
Carlo M.Croce
Yu-quan Wei
Chief-in-Editor：
Arnold J.M.Driessen
Yu-quan Wei
Chief-in-Editor：
James H.Naisimth
Yu-quan Wei
Journal
- MedComm Introduction
- Molecular Biomedicine Introduction
- Signal Transduction and Targeted Therapy Introduction
- MedComm | Incidence and risk factors of second primary cancer after the initial primary human papillomavirus related neoplasms
- Molecular Biomedicine | The bone marrow niche components are adversely affected in sepsis
The efficacy and synthetic versatility of asymmetric organocatalysis have contributed enormously to the field of organic synthesis since the early 2000s. As asymmetric organocatalytic methods mature, they have extended beyond the academia and undergone scale-up for the production of chiral drugs, natural products, and enantiomerically enriched bioactive molecules. This review provides a comprehensive overview of the applications of asymmetric organocatalysis in medicinal chemistry. A general picture of asymmetric organocatalytic strategies in medicinal chemistry is firstly presented, and the specific applications of these strategies in pharmaceutical synthesis are systematically described, with a focus on the preparation of antiviral, anticancer, neuroprotective, cardiovascular, antibacterial, and antiparasitic agents, as well as several miscellaneous bioactive agents. The review concludes with a discussion of the challenges, limitations and future prospects for organocatalytic asymmetric synthesis of medicinally valuable compounds.
Chemical Society Reviews
Chengdu University of Traditional Chinese Medicine
The COVID-19 pandemic caused by the SARS-CoV-2 virus continually poses serious threats to global public health. The main protease (Mpro) of SARS-CoV-2 plays a central role in viral replication. We designed and synthesized 32 new bicycloproline-containing Mpro inhibitors derived from either Boceprevir or Telaprevir, both of which are approved antivirals. All compounds inhibited SARS-CoV-2 Mpro activity in vitro with IC50 values ranging from 7.6 to 748.5 nM. The co-crystal structure of Mpro in complex with MI-23, one of the most potent compounds, revealed its interaction mode. Two compounds (MI-09 and MI-30) showed excellent antiviral activity in cell-based assays. In a SARS-CoV-2 infection transgenic mouse model, oral or intraperitoneal treatment with MI-09 or MI-30 significantly reduced lung viral loads and lung lesions. Both also displayed good pharmacokinetic properties and safety in rats.
Science
West China Hospital, SCU
