Role of the azinomycin naphthoate and central amide in sequence-dependent DNA alkylation and cytotoxicity of epoxide-bearing substructures

被引:28
作者
Coleman, RS
Burk, CH
Navarro, A
Brueggemeier, RW
Diaz-Cruz, ES
机构
[1] Ohio State Univ, Dept Chem, Columbus, OH 43210 USA
[2] Ohio State Univ, Coll Pharm, Columbus, OH 43210 USA
关键词
D O I
10.1021/ol0267275
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] Studies report a strong correlation between duplex DNA alkylation and in vitro cytotoxicity for a series of azinomycin partial structures 2-6 bearing the biologically relevant epoxide. Compounds lacking the naphthoate ester (e.g., 5 and 6) were poorly reactive toward DNA and were biologically inactive, as were compounds bearing the naphthoate but lacking the terminal carboxamide (e.g., 2). Compounds were evaluated for cytotoxicity against two breast cancer cell lines.
引用
收藏
页码:3545 / 3548
页数:4
相关论文
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