Journal
SYNLETT
Volume 28, Issue 20, Pages 2881-2885Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0036-1588539
Keywords
PROTAC; thalidomide; conjugates; linker; pentafluorophenyl ester
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Funding
- Multiple Myeloma Research Foundation
- NSERC
- University of Calgary
- Alberta Children's Hospital Foundation and Research Institute
- Charbonneau Cancer Institute
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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.
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