Atropisomerism in the Pharmaceutically Relevant Realm
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Abstract
> 4.5 years). In general, class-3 atropisomers are considered to be suitable for drug development. There are currently four FDA-approved drugs that exist as stable atropisomers, and many others are in clinical trials or have recently appeared in the drug discovery literature. Class-1 atropisomers are more prevalent, with ∼30% of recent FDA-approved small molecules possessing at least one class-1 axis. While class-1 atropisomers do not possess the requisite stereochemical stability to meet the classical definition of atropisomerism, they often bind a given target in a specific set of chiral conformations.Over the past decade, our laboratory has embarked on a research program aimed at leveraging atropisomerism…
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4Topics & keywords
Topics
Keywords
- Atropisomer
- Racemization
- Chemistry
- Axial chirality
- Chirality (physics)
- Stereochemistry
- Combinatorial chemistry
- Enantioselective synthesis
UN Sustainable Development Goals
- Good health and well-being
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