Synthesis and biological evaluation of antibody conjugates of phosphate prodrugs of cytotoxic DNA alkylators for the targeted treatment of cancer

RY Zhao, HK Erickson, BA Leece, EE Reid…

文献索引：Zhao, Robert Yongxin; Erickson, Hans K.; Leece, Barbara A.; Reid, Emily E.; Goldmacher, Victor S.; Lambert, John M.; Chari, Ravi V. J. Journal of Medicinal Chemistry, 2012 , vol. 55, # 2 p. 766 - 782

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被引用次数: 28

摘要

The synthesis and biological evaluation of phosphate prodrugs of analogues of 1 (CC-1065) and their conjugates with antibodies are described. The phosphate group on the 1, 2, 9, 9a- tetrahydrocyclopropa [c] benz [e] indol-4-one (CBI) portion of the compounds confers enhanced solubility and stability in aqueous solutions. In the presence of phosphatases, these compounds convert into active DNA-alkylating agents. The synthesis of the ...