期刊
CHEMMEDCHEM
卷 16, 期 19, 页码 3003-3016出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202100383
关键词
Antiproliferation; dibenzothiazines; drug design; sulfonamides; tubulin inhibitors
资金
- Agencia Cordoba Ciencia, Consejo Nacional de Investigaciones Cientificas y Tecnicas (CONICET)
- Secretaria de Ciencia y Tecnologia, Universidad Nacional de Cordoba (SECyT)
- Agencia Nacional de Promocion Cientifica y Tecnica (ANPCyT)
- CONICET
- Spanish Government [PGC2018-094503-B-C22]
- Ministerio de Ciencia e Innovacion [PID2019-10454RB-I00/AEI/10.13039/501100011033, 201920E111, 202020E301]
- Consejo Superior de Investigaciones Cientificas
- Fundacion TATIANA
- European Union [H2020-MSCA-ITN-2019 860070]
Researchers synthesized a series of potential anti-tumor dibenzothiazine compounds and identified two compounds with promising activity values. These compounds were shown to inhibit the proliferative activity of human solid tumor cells.
We prepared a series of free NH and N-substituted dibenzonthiazines with potential anti-tumor activity from N-aryl-benzenesulfonamides. A biological test of synthesized compounds (59 samples) was performed in vitro measuring their antiproliferative activity against a panel of six human solid tumor cell lines and its tubulin inhibitory activity. We identified 6-(phenylsulfonyl)-6H-dibenzo[c,e][1,2]thiazine 5,5-dioxide and 6-tosyl-6H-dibenzo[c,e][1,2]thiazine 5,5-dioxide as the best compounds with promising values of activity (overall range of 2-5.4 mu M). Herein, we report the dibenzothiazine core as a novel building block with antiproliferative activity, targeting tubulin dynamics.
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