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)May,, 2019, 25(26), 6500-6504 [doi].
    (last updated on 2024/04/24)

    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.