Design, Synthesis, and inâ
vitro Evaluation of Tubulin-Targeting Dibenzothiazines with Antiproliferative Activity as a Novel Heterocycle Building Block.
ChemMedChem
; 16(19): 3003-3016, 2021 10 06.
Article
em En
| MEDLINE
| ID: mdl-34231318
ABSTRACT
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 inâ
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 2-5.4â
µM). Herein, we report the dibenzothiazine core as a novel building block with antiproliferative activity, targeting tubulin dynamics.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiazinas
/
Tubulina (Proteína)
/
Desenho de Fármacos
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Moduladores de Tubulina
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Compostos Heterocíclicos
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Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
ChemMedChem
Ano de publicação:
2021
Tipo de documento:
Article