Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies
In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives ( 5a–g ) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer acti...
Saved in:
Published in | Journal of chemical biology Vol. 9; no. 4; pp. 97 - 106 |
---|---|
Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
Berlin/Heidelberg
Springer Berlin Heidelberg
01.10.2016
Springer Nature B.V |
Subjects | |
Online Access | Get full text |
Cover
Loading…
Summary: | In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives (
5a–g
) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound
5d
(NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound
5d
was active against all the cell lines, it has shown potential activity against leukemia SR (GI
50
: 2.04 μM), non-small cell lung cancer NCI-H522 (GI
50
: 1.36 μM), colon cancer COLO 205 (GI
50
: 1.64 μM), CNS cancer SF-539 (GI
50
: 1.87 μM), melanoma SK-MEL-2 (GI
50
: 1.64 μM), ovarian cancer OVCAR-3 (GI
50
: 1.87 μM), renal cancer RXF 393 (GI
50
: 1.15 μM), prostate cancer PC-3 (GI
50
: 1.90 μM), and breast cancer MDA-MB-468(GI
50
: 1.11 μM). DNA cleavage studies revealed that at 50 μg/mL concentration, partial DNA digestion was observed and when the concentration is increasing to threefold (150 μg/mL), complete linear DNA digestion and partial supercoiled DNA digestion was observed. Further antimicrobial studies indicate that all the synthesized compounds except compound
5a
possess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs. |
---|---|
Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 1864-6158 1864-6166 |
DOI: | 10.1007/s12154-016-0154-8 |