ACS Medicinal Chemistry Letters p. 1185 - 1190 (2020)
Update date:2022-08-29
Topics:
Bloomfield, Graham
Booker-Milburn, Kevin I.
Cox, Brian
Cox, Philip B.
Elliott, Luke D.
Paumier, Romain
Robertson-Ralph, Michael
Zdorichenko, Victor
The pressure to deliver new medicines to the patient continues to grow along with increases in compound failure rate, thus putting the current R&D model at risk. Analysis has shown that increasing the three-dimensionality of potential drug candidates decreases the risk of failure and improves binding selectivity and frequency. For this reason many workers have taken a new look at the power of photochemistry as a means to generate novel sp3 rich scaffolds for use in drug discovery programs. Here we report the design, synthesis, and computational structural analysis of a series of 2,4-methanoprolines having inherent 3D character (PMI and PBF scores) significantly higher than that of the broader AbbVie Rule of 3 (Ro3) collection.
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