Solid-Phase Synthesis of Duocarmycin Analogues and the Effect of C-Terminal Substitution on Biological Activity

…, C Adcock, J Kingston, H Sheldrake…

Index: Sheldrake, Helen M.; Travica, Sandra; Johansson, Inger; Loadman, Paul M.; Sutherland, Mark; Elsalem, Lina; Illingworth, Nicola; Cresswell, Alexander J.; Reuillon, Tristan; Shnyder, Steven D.; Mkrtchian, Souren; Searcey, Mark; Ingelman-Sundberg, Magnus; Patterson, Laurence H.; Pors, Klaus Journal of Medicinal Chemistry, 2013 , vol. 56, # 15 p. 6273 - 6277

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Abstract

The duocarmycins are potent antitumor agents with potential for use in the development of antibody–drug conjugates (ADCs) as well as being clinical candidates in their own right. In this article, we describe the synthesis of a duocarmycin monomer (DSA) that is suitably