A General Strategy for the Preparation of Thalidomide-Conjugate Linkers
Date
2017-01
Journal Title
Journal ISSN
Volume Title
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Abstract
The synthesis of small-molecule linkers for installation of thalidomide-based conjugates is described. Linker properties have been recognized as vital to conjugate success in drug discovery and delivery systems. These small-molecule tethers act as linkages between molecules, can also aid in cell permeability, and act as solubilizing agents. This work shows our progress in synthesizing conjugates with a variety of linker characteristics. The adaptability and manipulation of these and other linkers holds potential in improving synthetic control of chemical connectivities toward therapeutic development.
Description
Keywords
PROTAC, thalidomide, conjugates, linker, pentafluoroĀphenyl ester
Citation
Papatzimas, J. W., Gorobets, E., Brownsey, D. K., Maity, R., Bahlis, N. J., & Derksen, D. J. (2017). A general strategy for the preparation of thalidomide-conjugate linkers. Synlett, 28(20), 2881-2885.