A General Strategy for the Preparation of Thalidomide-Conjugate LinkersThis work was funded by the Multiple Myeloma Research Foundation, NSERC, the University of Calgary, Alberta Children’s Hospital Foundation and Research Institute, and the Charbonneau Cancer Institute.
Received: 26 May 2017
Accepted after revision: 17 July 2017
23 August 2017 (eFirst)
◊ These authors contributed equally
Dedicated to Victor Snieckus on the occasion of his 80th birthday
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.