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Escaping from flatland: [2 + 2] photocycloaddition; conformationally constrained sp3-rich scaffolds for lead generation

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posted on 2023-06-09, 22:27 authored by Brian Cox, Kevin I Booker-Milburn, Luke D Elliott, Michael Robertson-Ralph, Victor Zdorichenko
Pressure on researchers to deliver new medicines to the patient continues to grow. Attrition rates in the research and development process present a significant challenge to the viability of the current model of drug discovery. Analysis shows that increasing the three-dimensionality of potential drug candidates decreases the risk of attrition, and it is for this reason many workers have taken a new look at the power of photochemistry, in particular photocycloadditions, as a means to generate novel sp3-rich scaffolds for use in drug discovery programs. The viability of carrying out photochemical reactions on scale is also being addressed by the introduction of new technical developments.

History

Publication status

  • Published

File Version

  • Accepted version

Journal

ACS Medicinal Chemistry Letters

ISSN

1948-5875

Publisher

American Chemical Society

Issue

11

Volume

10

Page range

1512-1517

Event location

United States

Department affiliated with

  • Chemistry Publications

Full text available

  • Yes

Peer reviewed?

  • Yes

Legacy Posted Date

2020-12-15

First Open Access (FOA) Date

2020-12-15

First Compliant Deposit (FCD) Date

2020-12-14

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