Novel heterocyclic family of phenyl naphthothiazole carboxamides derived from naphthalimides: synthesis, antitumor evaluation, and DNA photocleavage |
| |
Authors: | Li Zhigang Yang Qing Qian Xuhong |
| |
Institution: | State Key Laboratory of Fine Chemicals, Dalian University of Technology, Dalian 116012, China. |
| |
Abstract: | A new heterocyclic family of (2-(dimethylamino)ethyl)-2-substituted phenylnaphtho2,1-d]thiazole-5-carboxamides modified from naphthalimides was designed, synthesized, and quantitatively evaluated as antitumor agents and photonucleases. All these compounds were found to be more cytotoxic against P388 than against A549. B(3) (m-NO(2)) was found to be the strongest inhibitor for P388 with IC(50) of 1.49 microM, while B(2) was the most cytotoxic compound against A549 with IC(50) of 12 microM. B(4) (p-CH(3)), the most efficient DNA photocleaver, showed detectable DNA cleavage at 0.5 microM and total cleavage from form I to 100% form II at 50 microM. The photocleaving mechanism was changed with the modification to be via superoxide anion and radical. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|