Escaping from flatland: [2 + 2] photocycloaddition; conformationally constrained sp<sup>3</sup>-rich scaffolds for lead generation

Cox, Brian, Booker-Milburn, Kevin I, Elliott, Luke D, Robertson-Ralph, Michael and Zdorichenko, Victor (2019) Escaping from flatland: [2 + 2] photocycloaddition; conformationally constrained sp<sup>3</sup>-rich scaffolds for lead generation. ACS Medicinal Chemistry Letters, 10 (11). pp. 1512-1517. ISSN 1948-5875

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Abstract

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.

Item Type: Article
Keywords: Drug discovery, photocycloaddition, sp(3)-rich scaffolds, hit and lead generation
Schools and Departments: School of Life Sciences > Chemistry
SWORD Depositor: Mx Elements Account
Depositing User: Mx Elements Account
Date Deposited: 15 Dec 2020 10:36
Last Modified: 15 Dec 2020 10:45
URI: http://sro.sussex.ac.uk/id/eprint/95714

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