Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues.
Bioorg Med Chem
; 21(24): 7624-7, 2013 Dec 15.
Article
in En
| MEDLINE
| ID: mdl-24262885
ABSTRACT
In an effort to develop potent anti-cancer chemopreventive agents that act on topoisomerase II, a novel series of bisindolylalkanes analogues such as 3,3'-(thiochroman-4,4-diyl)bis(1H-indole) are synthesized. Structures of all compounds are elucidated by (1)H NMR, (13)C NMR and HRMS. Anti-proliferative activities for all of these compounds are investigated by the method of MTT assay on 7 human cancer lines. Most of them showed antitumor activities in vitro, the half maximal inhibitory concentration (IC50) value is 7.798 µg/mL of 3a against MCF7. Compound 3a showed comparable topoisomerase II inhibitory activity to etoposide (VP-16) at 100 µM concentration. The rest of the compounds also showed varying degree topoisomerase II inhibitory activity.
Key words
Full text:
1
Database:
MEDLINE
Main subject:
DNA Topoisomerases, Type II
/
Topoisomerase II Inhibitors
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Indoles
Limits:
Humans
Language:
En
Year:
2013
Type:
Article