title: Synthesis of thiazolidine-2,4-dione derivatives: anticancer, antimicrobial and DNA cleavage studies.
abstract: 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 compound5d(NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound5dwas active against all the cell lines, it has shown potential activity against leukemia SR (GI50: 2.04 μM), non-small cell lung cancer NCI-H522 (GI50: 1.36 μM), colon cancer COLO 205 (GI50: 1.64 μM), CNS cancer SF-539 (GI50: 1.87 μM), melanoma SK-MEL-2 (GI50: 1.64 μM), ovarian cancer OVCAR-3 (GI50: 1.87 μM), renal cancer RXF 393 (GI50: 1.15 μM), prostate cancer PC-3 (GI50: 1.90 μM), and breast cancer MDA-MB-468(GI50: 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 compound5apossess prominent activity against all the screened microbial species. This study throws a ray of light in the field of anticancer drugs.
authors.affiliation: Department of Chemistry, K L University, Guntur, 522502 India.
authors.forename: S Vijaya
authors.initials: SV
authors.lastname: Laxmi
authors.affiliation: Department of Chemistry, K L University, Guntur, 522502 India.
authors.forename: P
authors.initials: P
authors.lastname: Anil
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal, 506004 India.
authors.forename: G
authors.initials: G
authors.lastname: Rajitha
authors.affiliation: Department of Zoology, Bhavan's College, Andheri(W), Mumbai, 400058 India.
authors.forename: Asha Jyothi
authors.initials: AJ
authors.lastname: Rao
authors.affiliation: Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for medical Sciences, Little Rock, AR 72205 USA.
authors.forename: Peter A
authors.initials: PA
authors.lastname: Crooks
authors.affiliation: Department of Chemistry, National Institute of Technology, Warangal, 506004 India.
authors.forename: B
authors.initials: B
authors.lastname: Rajitha
keywords: 4-dione; 4-hydroxybenzyledenethiazolidine-2; Anticancer activity; Antimicrobial activity; Cancer; DNA cleavages studies