Synthesis and cytotoxic activity of novel hexahydropyrrolo[2,3-b]indole imidazolium salts.
Bioorg Med Chem Lett
; 26(2): 460-465, 2016 Jan 15.
Article
in En
| MEDLINE
| ID: mdl-26684853
ABSTRACT
A series of novel hexahydropyrrolo[2,3-b]indole-1H-imidazolium salts were synthesized and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 5,6-dimethyl-benzimidazole ring, and substitution of the imidazolyl-3-position with a 2-bromobenzyl or 2-naphthylmethyl group, were important for the cytotoxic activity. Notably, Compound 43, bearing a 2-bromobenzyl substituent at position-3 of 5,6-dimethyl-benzimidazole, was found to possess the most potent derivative against five human tumor cell lines with IC50 values below 2.68µM and more selective towards SMMC-7721, A549 and SW480 cell lines. Compounds 25 and 39 were more selective to HL-60 and MCF-7 cell lines with IC50 values of 0.47 and 1.46µM.
Key words
Full text:
1
Database:
MEDLINE
Main subject:
Pyrroles
/
Imidazoles
/
Indoles
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Year:
2016
Type:
Article