The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase

X Zhang, B Bao, X Yu, L Tong, Y Luo, Q Huang…

Index: Zhang, Xuan; Bao, Bin; Yu, Xiuhua; Tong, Linjiang; Luo, Yu; Huang, Qingqing; Su, Mingbo; Sheng, Li; Li, Jia; Zhu, Hong; Yang, Bo; Zhang, Xiongwen; Chen, Yi; Lu, Wei Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 22 p. 6981 - 6995

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Citation Number: 19

Abstract

Abstract A novel class of podophyllotoxin derivatives have been designed and synthesized based on the synergistic antitumor effects of topoisomerase II and histone deacetylase inhibitors. Their inhibitory activities towards histone deacetylases and Topo II and their cytotoxicities in cancer cell lines were evaluated. The aromatic capping group connection, linker length and zinc-binding group were systematically varied and preliminary ...