Synthesis of neolignans as microtubule stabilisers.
Bioorg Med Chem
; 22(4): 1342-54, 2014 Feb 15.
Article
em En
| MEDLINE
| ID: mdl-24457094
ABSTRACT
Tubulin is a well established target for anticancer drug development. Lignans and neolignans were synthesized as tubulin interacting agents. Neolignans 10 and 19 exhibited significant anticancer activity against MCF-7 and MDAMB-231 human breast cancer cell lines. Both the compounds effectively induced stabilization of microtubule at 4 and 20 µM concentrations respectively. Neolignan 10 induced G2/M phase arrest in MCF-7 cells. Docking experiments raveled that 10 and 19 occupied the same binding pocket of paclitaxel with some difference in active site amino acids and good bioavailability of both the compounds. In in vivo acute oral toxicity 10 was well tolerated up to 300 mg/kg dose in Swiss-albino mice.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tubulina (Proteína)
/
Lignanas
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Ácidos Cumáricos
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Antineoplásicos
Limite:
Animals
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Female
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Humans
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Male
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Índia