Publications [#342638] of Emily R. Derbyshire

Journal Articles

1. Lee, H; Sylvester, K; Derbyshire, ER; Hong, J, Synthesis and Analysis of Natural-Product-Like Macrocycles by Tandem Oxidation/Oxa-Conjugate Addition Reactions., Chemistry (Weinheim an der Bergstrasse, Germany), vol. 25 no. 26 (May, 2019), pp. 6500-6504 [doi]
   (last updated on 2024/12/31)

   Abstract:
   As traditional small-molecule drug discovery programs focus on a relatively narrow range of chemical space, most human proteins are viewed as unreachable targets. Consequently, there is a strong interest in expanding the chemical space in drug discovery beyond traditional small molecules. Here, a strategy for the preparation of a broad natural-product-like macrocyclic library by using the tandem allylic oxidation/oxa-conjugate addition and macrocyclization reactions is reported. Cheminformatic analyses demonstrate that this tetrahydropyran-containing macrocyclic library shows a significant overlap with natural products in the chemical space. This approach can be used for designing libraries that may probe more deeply into natural-product-like space.