Preliminary investigation of cytotoxic potential of 2-quinolone derivatives using in vitro and in vivo (solid tumor and liquid tumor) models of cancer

• Main Authors: Nitesh Kumar, Isha Dhamija, P. Vasanth Raj, B.S. Jayashree, Vipan Parihar, S.N. Manjula, Seeja Thomas, N. Gopalan Kutty, C. Mallikarjuna Rao
• Format: Article
• Language: English
• Published: Elsevier 2014-09-01
• Series: Arabian Journal of Chemistry
• Subjects: Cytotoxicity; Cancer; 2-Quinolone; Solid tumor; Liquid tumor
• Online Access: http://www.sciencedirect.com/science/article/pii/S1878535212003206
• ISSN: 1878-5352

2-Quinolone analogs are powerful inhibitors of farnesyl transferase, and are a novel class of anticancer drugs. The present study focused on continual efforts to elucidate the anticancer activity of synthesized 2-quinolone derivatives without N-methyl or 3-aryl substitution. Three derivatives namely JST, JST2 and JST13 were synthesized in our lab and screened for in vitro and in vivo anticancer activities. Significant cytotoxicity was observed in MCF-7 cells treated with JST2 and JST13. Both the derivatives’ treatment showed damage to the DNA. In vivo studies for JST2 and JST13 were performed at two doses 100 and 200 mg/kg using Ehrlich ascites carcinoma (liquid) and Dalton lymphoma ascites (solid) models. Both derivatives showed a significant reduction in the tumor progression by increasing the mean life span and by improving the haematological profile and antioxidant status of the liver in a liquid tumor model. More prominent effect was observed in a solid tumor model by reduction in solid tumor weight and tumor volume.