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Facile synthesis of novel quinoline derivatives as anticancer agents

Abstract

Convenient and efficient synthesis of novel N-(4-acetyl-4,5-dihydro-5-(7,8,9-substituted-tetrazolo[1,5-a]-quinolin-4-yl)-1,3,4-thiadiazol-2-yl)acetamides 4aj and their in vitro anticancer activity against two cell lines viz., human breast cancer cell line MCF7 and human cervix cancer cell line HeLa were carried out. GI50, LC50, TGI values were evaluated. Two of the compounds 4e and 4i with halogen substituent at 7th position of the target molecules have shown potent activity against human cervix cancer cell line HeLa. DNA cleavage studies revealed that most of these compounds show partial cleavage and few of them show complete cleavage of DNA.

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Acknowledgments

The authors thank ACTREC, Mumbai and Biogenics, Hubballi, for assistance in conducting pharmacological assay and USIC, Karnatak University Dharwad—580003 for spectral characterization.

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Correspondence to Ravindra Ramappa Kamble.

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Marganakop, S.B., Kamble, R.R., Hoskeri, J. et al. Facile synthesis of novel quinoline derivatives as anticancer agents. Med Chem Res 23, 2727–2735 (2014). https://doi.org/10.1007/s00044-013-0855-2

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Keywords

  • Anticancer activity
  • Breast cancer cell line MCF7
  • Cervix cancer cell line HeLa
  • DNA cleavage
  • Quinoline