Azinomycin inspired bisepoxides: influence of linker structure on in vitro cytotoxicity and DNA interstrand cross-linking

作者：LePla RC; Landreau CAS; Shipman M^*; Hartley JA; Jones GDD

来源：Bioorganic & Medicinal Chemistry Letters, 2005, 15(11): 2861-2864.

DOI：10.1016/j.bcml.2005.03.091

• epoxides
• DNA alkylation
• interstrand cross-linking
• anti-cancer

A series of bisepoxides based on the epoxide domain of the naturally occurring azinomycins have been synthesised. The incorporation of an aminomethyl group into the linker between the two alkylating epoxide units is shown to significantly enhance in vitro cytotoxicity against human tumour cell lines and DNA interstand cross-linking efficiency.

• 出版日期2005-6-2