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

Nitesh Kumar, Isha Dhamija, P. Vasanth Raj, B. S. Jayashree, Vipan Parihar, S. N. Manjula, Seeja Thomas, N. Gopalan Kutty, C. Mallikarjuna Rao

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)409-417
Number of pages9
JournalArabian Journal of Chemistry
Volume7
Issue number4
DOIs
Publication statusPublished - 2014

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Tumors
Derivatives
Liquids
Cytotoxicity
Transferases
Antioxidants
Liver
DNA
Substitution reactions
carbostyril
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Chemical Engineering(all)

Cite this

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title = "Preliminary investigation of cytotoxic potential of 2-quinolone derivatives using in vitro and in vivo (solid tumor and liquid tumor) models of cancer",
abstract = "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.",
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Preliminary investigation of cytotoxic potential of 2-quinolone derivatives using in vitro and in vivo (solid tumor and liquid tumor) models of cancer. / Kumar, Nitesh; Dhamija, Isha; Vasanth Raj, P.; Jayashree, B. S.; Parihar, Vipan; Manjula, S. N.; Thomas, Seeja; Gopalan Kutty, N.; Mallikarjuna Rao, C.

In: Arabian Journal of Chemistry, Vol. 7, No. 4, 2014, p. 409-417.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Preliminary investigation of cytotoxic potential of 2-quinolone derivatives using in vitro and in vivo (solid tumor and liquid tumor) models of cancer

AU - Kumar, Nitesh

AU - Dhamija, Isha

AU - Vasanth Raj, P.

AU - Jayashree, B. S.

AU - Parihar, Vipan

AU - Manjula, S. N.

AU - Thomas, Seeja

AU - Gopalan Kutty, N.

AU - Mallikarjuna Rao, C.

PY - 2014

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N2 - 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.

AB - 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.

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