Mimicking the biological activity of diazobenzo[b]fluorene natural products with electronically tuned diazofluorene analogs
作者:Wei Zeng、T. Eric Ballard、Alexander G. Tkachenko、Virginia A. Burns、Daniel L. Feldheim、Christian Melander
DOI:10.1016/j.bmcl.2006.07.024
日期:2006.10
Under appropriate electronic modulation, simple diazofluorene analogs recapitulate the DNA cleavage activity of kinamycin D under thiol-based reducing conditions. Achieving DNA cleavage under these reducing conditions is key to anticancer activity, as the most active compound, 1-methoxydiazofluorene, inhibits the proliferation of HeLa cells.
在适当的电子调制下,简单的重氮芴类似物在基于硫醇的还原条件下概括了凯那霉素D的DNA裂解活性。在这些还原条件下实现DNA裂解是抗癌活性的关键,因为最具活性的化合物1-甲氧基重氮芴可抑制HeLa细胞的增殖。