文献类型：期刊文献

英文题名：Oxo-heterocyclic fused naphthalimides as antitumor agents: Synthesis and biological evaluation

作者：Tan, Shaoying[1,4];Yin, Hong[2,4];Chen, Zhuo[3,4];Qian, Xuhong[1,2,4];Xu, Yufang[1,2,3,4]

机构：[1]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[2]E China Univ Sci & Technol, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[3]E China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China;[4]E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

年份：2013

卷号：62

起止页码：130

外文期刊名：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000318577500014)】；

基金：This work is financially supported by the National Basic Research Program of China (973 Program, 2010CB126100), the National High Technology Research and Development Program of China (863 Program, 2011AA10A207), the China 111 Project (grant B07023), the Fundamental Research Funds for the Central Universities, and the Shanghai Committee of Science and Technology [grant 11DZ2260600]. We thank Chenghui Xu for antiproliferation assay against A549 and P388 cancer cell lines.

语种：英文

外文关键词：Oxo-heterocyclic; Naphthalimides; Antitumor agents; Topo I; Topo II; DNA intercalation

摘要：Three series of novel oxo-heterocyclic fused naphthalimide derivatives (8a-8f, 13a-13d, 17a-17d) were prepared. The newly-synthesized compounds, and their thio-heterocyclic fused analogs (1a-1c, 2a-2d, 3a-3c) exhibited potent antiproliferative activity correlated well with their structure. Further research demonstrated that all the representative compounds 13a, 2a and 17a, 3a showed strong inhibition activity to topo II similarly with amonafide, and also potent topo I inhibition activity, which was seldom reported before for naphthalimide derivatives. Preliminary exploration proved their DNA sequence preference. In all, dual topo I/topo II inhibition and DNA sequence preference might contribute to enhancing tumor selectivity and overcoming drug resistance. (C) 2013 Elsevier Masson SAS. All rights reserved.