Synthesis and antitumor effects of novel benzyl naphthyl sulfoxide/sulfone derivatives derived from Rigosertib |
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| Authors: | Lin Tang Tingting Chen Hongpeng Yang Xiaoxue Wen Yunbo Sun Shuchen Liu Tao Peng Shouguo Zhang Lin Wang |
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| Institution: | Beijing Institute of Radiation Medicine, Beijing 100850 P. R. China, +86 010 66932239 ; Faculty of Environment & Life, Beijing University of Technology, Beijing 100124 P. R. China |
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| Abstract: | In this work, a series of novel benzyl naphthyl sulfoxides/sulfones derived from Rigosertib were designed and synthesized as potential antitumor agents. The in vitro cytotoxicity against four human cancer cell lines (HeLa, MCF-7, HepG2 and SCC-15) and two normal human cell lines (HUVEC and 293T) indicated that some of the sulfones and sulfoxides possessed potent antineoplastic activity that reached nanomolar levels and relatively low toxicity to normal cells. Among them, (2-methoxy-5-((naphthalen-2-ylsulfonyl)methyl)phenyl)glycine (15b) was found to be a promising antitumor drug candidate that could significantly inhibit tumor cell migration and induce tumor cell apoptosis via the p53-Bcl-2-Bax signaling pathway at nanomolar concentrations.In this work, a series of novel benzyl naphthyl sulfoxides/sulfones derived from Rigosertib were designed and synthesized as potential antitumor agents. |
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