Open AccessEscaping from Flatland: [2 + 2] Photocycloaddition; Conformationally Constrained sp3-rich Scaffolds for Lead Generation
Author(s) -
Brian J. Cox,
Kevin I. BookerMilburn,
Luke D. Elliott,
Michael Robertson-Ralph,
Victor Zdorichenko
Publication year - 2019
Publication title -
acs medicinal chemistry letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.065
H-Index - 66
ISSN - 1948-5875
DOI - 10.1021/acsmedchemlett.9b00409
Subject(s) - attrition , lead (geology) , drug discovery , computer science , process (computing) , nanotechnology , chemistry , data science , materials science , medicine , biology , paleontology , biochemistry , dentistry , operating system
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 sp 3 -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.