Novel quinolone substituted thiazolidin-4-ones as anti-inflammatory, anticancer agents: Design, synthesis and biological screening

作者：Suthar Sharad Kumar; Jaiswal Varun; Lohan Sandeep; Bansal Sumit; Chaudhary Anil; Tiwari Amit; Alex Angel Treasa; Joesph Alex^*

来源：European Journal of Medicinal Chemistry, 2013, 63: 589-602.

DOI：10.1016/j.ejmech.2013.03.011

• Quinolone
• Thiazolidin-4-one
• NF-kappa B
• Docking
• Anti-inflammatory
• Anticancer

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

• 出版日期2013-5