Nitro and amino substitution within the A-ring of 5H-8, 9-dimethoxy-5-(2-N, N-dimethylaminoethyl) dibenzo [c, h][1, 6] naphthyridin-6-ones: influence on topoisomerase …
AL Ruchelman, JE Kerrigan, TK Li, N Zhou…
文献索引:Ruchelman, Alexander L.; Kerrigan, John E.; Li, Tsai-Kun; Zhou, Nai; Liu, Angela; Liu, Leroy F.; LaVoie, Edmond J. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 13 p. 3731 - 3742
Recently, 5H-8, 9-dimethoxy-5-(2-N, N-dimethylaminoethyl)-2, 3-methylenedioxydibenzo [c, h][1, 6] naphthyridin-6-one, 1, was identified as a TOP1-targeting agent with pronounced antitumor activity. In the present study, the effect on activity of substituting a single nitro or amino group in the A-ring in lieu of the methylenedioxy moiety of 1 was evaluated. The presence of either a nitro or amino substituent at the 4-position had a pronounced adverse ...