Synthesis and cytotoxicity of novel simplified eleutherobin analogues as potential antitumour agents.
Org Biomol Chem
; 17(10): 2792-2797, 2019 03 06.
Article
em En
| MEDLINE
| ID: mdl-30793716
ABSTRACT
Mixed simplified structures containing the paclitaxel and eleutherobin pharmacophore moieties were analyzed using molecular docking techniques and synthesized based on adamantane and 8-oxabicyclo[3.2.1]octane scaffolds. The crucial role of substituents' stereochemistry in biological activity is discussed. At micromolar concentrations the selected analogues interfered with tubulin dynamics in vitro and in a living organism. Furthermore, new compounds were cytotoxic against human tumour cell lines. The simplified eleutherobin analogues may be considered as prototypes of a new class of antitumour agents.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Diterpenos
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Org Biomol Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2019
Tipo de documento:
Article
País de afiliação:
Federação Russa