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Synthesis, DNA binding, docking and photocleavage studies of quinolinyl chalcones

Bindu, PJ and Mahadevan, KM and Naik, Ravikumar TR and Harish, BG (2014) Synthesis, DNA binding, docking and photocleavage studies of quinolinyl chalcones. In: MEDCHEMCOMM, 5 (11). pp. 1708-1717.

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Official URL: http://dx.doi.org/ 10.1039/c4md00185k


A series of simple quinoline-chalcone conjugates have been synthesized by Claisen-Schmidt condensation reactions of substituted acetophenones with 2-chloro-3-formyl-quinoline and evaluated for their nucleolytic activity. The structures of the synthesized quinoline-chalcone conjugates were confirmed by IR, H-1 NMR, C-13 NMR and mass spectral analyses. Most of the prepared compounds showed significant DNA binding and photocleavage activities. The incorporation of an electron-donating group into ring A caused a moderate increase in the DNA binding and photocleavage activities. Compounds 3c and 3d exhibited promising DNA photocleavage against pUC 19 DNA with 85% inhibition at 100 mu M concentration. A structure-activity relationship analysis of these compounds was performed; compounds 3c and 3d are potential candidates for future drug discovery and development.

Item Type: Journal Article
Publication: MEDCHEMCOMM
Additional Information: Copyrights for this articles belong to the ROYAL SOC CHEMISTRY, THOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLAND
Department/Centre: Division of Interdisciplinary Sciences > Centre for Nano Science and Engineering
Date Deposited: 14 Dec 2014 10:20
Last Modified: 14 Dec 2014 10:20
URI: http://eprints.iisc.ac.in/id/eprint/50431

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