Novel Quinolone Substituted Thiazolidin-4-ones as Anti-in Flammatory, Anticancer Agents: Design, Synthesis and Biological Screening

Suthar, Sharad Kumar and Lohan, Sandeep and Bansal, Sumit and Chaudhary, Anil and Tiwari, Amit and Alex, Angel Treasa and Joesph, Alex (2013) Novel Quinolone Substituted Thiazolidin-4-ones as Anti-in Flammatory, Anticancer Agents: Design, Synthesis and Biological Screening. European Journal of Medicinal Chemistry, 63. pp. 589-602.

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Abstract

Nuclear factor-kappaB (NF- kB) has been reported to regulate various genes involved in cancer and in flammation. Accordingly, drugs suppressing or inhibiting NF- kB may possess both anti-in flammatory and anticancer properties. A library of quinolone substituted thiazolidin-4-ones was docked into the active site of NF- kB and the top-ranked 31 compounds were synthesized and evaluated for anti-in flammatory and anticancer activity. The best-ranked compound 6b showed highest anti-in flammatory activity in carrageenan-induced paw edema model. In vitro anticancer studies revealed 1a and 16a as most active compounds against BT-549, HeLa, COLO-205 and ACHN human cancer cell lines. Compounds 1a and 16a exhibited NF-kB dependent anticancer properties and apoptosis mediated cell death. In vivo Ehrlich ascites carcinoma study further con firmed the antitumor activity of 1a and 16a.

Item Type: Article
Uncontrolled Keywords: Quinolone; Thiazolidin-4-one; NF-k B; Docking; Anti-in flammatory; Anticancer
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Biotechnology
Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Manipal
Date Deposited: 07 Dec 2013 04:30
Last Modified: 07 Dec 2013 04:30
URI: http://eprints.manipal.edu/id/eprint/137924

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