Dipeptide-based highly potent doxorubicin antibody conjugates

SC Jeffrey, MT Nguyen, JB Andreyka, DL Meyer…

Index: Jeffrey, Scott C.; Nguyen, Minh T.; Andreyka, Jamie B.; Meyer, Damon L.; Doronina, Svetlana O.; Senter, Peter D. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 2 p. 358 - 362

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Citation Number: 39

Abstract

Highly potent and novel derivatives of doxorubicin were linked to monoclonal antibodies (mAbs) for site-specific drug delivery. Drug linker 5 consisted of a dipeptide linker attached directly to the daunosamine nitrogen of the n-butyldiacetate doxorubicin derivative 2a. Upon hydrolysis of the peptide linker and acetate groups, the free daunosamine nitrogen is able to form the highly potent 2-pyrrolinodoxorubicin (3a). The second approach involved the use ...