Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents |
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| Authors: | Haosha Tang Yunyan Kuang Julan Zeng Xiaofang Li Wei Zhou Yuan Lu |
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| Affiliation: | Obstetrics and Gynecology Hospital, Fudan University, 419 Fangxie Road, Shanghai 200011 China ; Department of Chemistry, Fudan University, 2005 Songhu Road, Shanghai 200433 China.; Department of Chemistry, Changsha University of Science and Technology, Changsha 410114 China ; School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201 China |
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| Abstract: | ![]()
Combinatorial synthesis of (E)-β-trifluoromethyl vinylsulfones is accomplished through a reaction of alkynes, Togni reagent, and sodium benzenesulfinates in DMSO under metal-free conditions at room temperature. These compounds are evaluated in several assays against different tumor cells. Some hits are identified against ES-2, HO-8910, and K562.(E)-β-Trifluoromethyl vinylsulfones is accomplished through a reaction of alkynes, Togni reagent, and sodium benzenesulfinates under metal-free conditions. p-Acetylphenyl in R1 has the best activities against several tumor cells. |
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