Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents

Haosha Tang; Yunyan Kuang; Julan Zeng; Xiaofang Li; Wei Zhou; Yuan Lu

doi:10.1039/C9RA06368D

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Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents†

Haosha Tang,^a Yunyan Kuang,^b Julan Zeng,^c Xiaofang Li,^d Wei Zhou

*^b and Yuan Lu*^a

Author affiliations

* Corresponding authors

^a Obstetrics and Gynecology Hospital, Fudan University, 419 Fangxie Road, Shanghai 200011, China

^b Department of Chemistry, Fudan University, 2005 Songhu Road, Shanghai 200433, China
E-mail: zhouw@fudan.edu.cn

^c Department of Chemistry, Changsha University of Science and Technology, Changsha 410114, China

^d School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, China

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.

This article is part of the themed collection: Editors' Collection: Fluorine chemistry in medicinal chemistry and chemical biology

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Article information

DOI: https://doi.org/10.1039/C9RA06368D
Article type: Paper
Submitted: 15 Aug 2019
Accepted: 26 Sep 2019
First published: 03 Oct 2019
This article is Open Access

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RSC Adv., 2019,9, 31474-31482

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Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents

H. Tang, Y. Kuang, J. Zeng, X. Li, W. Zhou and Y. Lu, RSC Adv., 2019, 9, 31474 DOI: 10.1039/C9RA06368D

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Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents†

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Combinatorial synthesis and biological evaluations of (E)-β-trifluoromethyl vinylsulfones as antitumor agents

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