Open AccessSynthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies
Author(s) -
S. Vijaya Laxmi,
Pandit Anil,
Galla Rajitha,
Asha Jyothi Rao,
Peter A. Crooks,
B. Rajitha
Publication year - 2016
Publication title -
journal of chemical biology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.355
H-Index - 24
eISSN - 1864-6166
pISSN - 1864-6158
DOI - 10.1007/s12154-016-0154-8
Subject(s) - antimicrobial , chemistry , dna , melanoma , cleavage (geology) , cancer , cancer research , cell cycle , microbiology and biotechnology , cell , biochemistry , biology , medicine , organic chemistry , paleontology , fracture (geology)
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.