Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer

A series of tertiary sulphonamide derivatives were synthesised and evaluated for their antiproliferative activity against liver cancer cell lines (SNU-475, HepG-2, and Bel-7402). Among these tertiary sulphonamides, compound 17a displayed the best anti-liver cancer activity against Bel-7402 cells wit...

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Main Authors:	Lijuan Ding, Feng Wei, Nanya Wang, Yue Sun, Qiang Wang, Xia Fan, Ling Qi, Shudong Wang
Format:	Article
Language:	English
Published:	Taylor & Francis Group 2021-01-01
Series:	Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:	tertiary sulphonamide liver cancer bel-7402 cells tubulin polymerisation lsd1
Online Access:	http://dx.doi.org/10.1080/14756366.2021.1917564

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spelling	doaj-a2a2cf292d1e49e6bd72a3de452c6c6a2021-07-26T12:59:35ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742021-01-013611563157210.1080/14756366.2021.19175641917564Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancerLijuan Ding0Feng Wei1Nanya Wang2Yue Sun3Qiang Wang4Xia Fan5Ling Qi6Shudong Wang7The First Hospital of Jilin UniversityThe First Hospital of Jilin UniversityThe First Hospital of Jilin UniversityThe First Hospital of Jilin UniversityThe First Hospital of Jilin UniversityThe First Hospital of Jilin UniversityThe Sixth Affiliated Hospital of Guangzhou Medical University, Qingyuan People’s HospitalThe First Hospital of Jilin UniversityA series of tertiary sulphonamide derivatives were synthesised and evaluated for their antiproliferative activity against liver cancer cell lines (SNU-475, HepG-2, and Bel-7402). Among these tertiary sulphonamides, compound 17a displayed the best anti-liver cancer activity against Bel-7402 cells with an IC50 value of 0.32 μM. Compound 17a could effectively inhibit tubulin polymerisation with an IC50 value of 1.27 μM. Meanwhile, it selectively suppressed LSD1 with an IC50 value of 63 nM. It also concentration-dependently inhibited migration against Bel-7402 cells. Importantly, tertiary sulphonamide 17a exhibited the potent antitumor activity in vivo. All these findings revealed that compound 17a might be a tertiary sulphonamide-based dual inhibitor of tubulin polymerisation and LSD1 to treat liver cancer.http://dx.doi.org/10.1080/14756366.2021.1917564tertiary sulphonamideliver cancerbel-7402 cellstubulin polymerisationlsd1
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Lijuan Ding Feng Wei Nanya Wang Yue Sun Qiang Wang Xia Fan Ling Qi Shudong Wang
spellingShingle	Lijuan Ding Feng Wei Nanya Wang Yue Sun Qiang Wang Xia Fan Ling Qi Shudong Wang Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer Journal of Enzyme Inhibition and Medicinal Chemistry tertiary sulphonamide liver cancer bel-7402 cells tubulin polymerisation lsd1
author_facet	Lijuan Ding Feng Wei Nanya Wang Yue Sun Qiang Wang Xia Fan Ling Qi Shudong Wang
author_sort	Lijuan Ding
title	Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer
title_short	Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer
title_full	Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer
title_fullStr	Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer
title_full_unstemmed	Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer
title_sort	tertiary sulphonamide derivatives as dual acting small molecules that inhibit lsd1 and suppress tubulin polymerisation against liver cancer
publisher	Taylor & Francis Group
series	Journal of Enzyme Inhibition and Medicinal Chemistry
issn	1475-6366 1475-6374
publishDate	2021-01-01
description	A series of tertiary sulphonamide derivatives were synthesised and evaluated for their antiproliferative activity against liver cancer cell lines (SNU-475, HepG-2, and Bel-7402). Among these tertiary sulphonamides, compound 17a displayed the best anti-liver cancer activity against Bel-7402 cells with an IC50 value of 0.32 μM. Compound 17a could effectively inhibit tubulin polymerisation with an IC50 value of 1.27 μM. Meanwhile, it selectively suppressed LSD1 with an IC50 value of 63 nM. It also concentration-dependently inhibited migration against Bel-7402 cells. Importantly, tertiary sulphonamide 17a exhibited the potent antitumor activity in vivo. All these findings revealed that compound 17a might be a tertiary sulphonamide-based dual inhibitor of tubulin polymerisation and LSD1 to treat liver cancer.
topic	tertiary sulphonamide liver cancer bel-7402 cells tubulin polymerisation lsd1
url	http://dx.doi.org/10.1080/14756366.2021.1917564
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Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer

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