Synlett
DOI: 10.1055/s-0036-1588539
letter
© Georg Thieme Verlag Stuttgart · New York

A General Strategy for the Preparation of Thalidomide-Conjugate Linkers

James W. Papatzimasa, Evgueni Gorobetsa, Duncan K. Brownseya, Ranjan Maityb, Nizar J. Bahlisb, Darren J. Derksen*a
  • aDepartment of Chemistry, University of Calgary, 2500 University Drive NW, Calgary, Alberta, T2N 1N4, Canada   Email: dderksen@ucalgary.ca
  • bDepartment of Hematology and Oncology, University of Calgary, Calgary, Alberta, T2N 4N1, Canada
This 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.
Further Information

Publication History

Received: 26 May 2017

Accepted after revision: 17 July 2017

Publication Date:
23 August 2017 (eFirst)

These authors contributed equally

Dedicated to Victor Snieckus on the occasion of his 80th birthday

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.

Supporting Information