Unsymmetrical DNA cross-linking agents: combination of the CBI and PBD pharmacophores

M Tercel, SM Stribbling, H Sheppard…

文献索引：Tercel, Moana; Stribbling, Stephen M.; Sheppard, Hilary; Siim, Bronwyn G.; Wu, Kent; Pullen, Susan M.; Botting, K. Jane; Wilson, William R.; Denny, William A. Journal of Medicinal Chemistry, 2003 , vol. 46, # 11 p. 2132 - 2151

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被引用次数: 67

摘要

A set of 10 compounds, each combining the seco-1, 2, 9, 9a-tetrahydrocyclopropa [c] benz [e] indol-4-one (seco-CBI) and pyrrolo [2, 1-c][1, 4] benzodiazepine (PBD) pharmacophores, was designed and prepared. These compounds were anticipated to cross-link between N3 of adenine and N2 of guanine in the minor groove of DNA. The compounds, which differ in the chain length separating the two alkylation subunits, and the configuration of the CBI ...