Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 22, Issue 5, Pages 2360-2375Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-012-0230-8
Keywords
Naphthalimides; Cyclic imides; Synthesis; Antibacterial activity; Antitumor evaluation; Molecular modeling; Modeling
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Funding
- King Saud University [RGP-VPP-163]
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Carboxylic acid imides 1-26 have been synthesized and screened for their antibacterial against gram-positive and gram-negative organisms and their antitumor activity against 60 tumor cell lines taken from nine different organs. Compounds 12, 14, and 16 were the most active and broad-spectrum antibacterial member in this study. Compound 9 showed the most cytotoxicity with a significant inhibition for renal cancer cells. 2D-QSAR study provides details on the fine relationship linking structure and activity and offers clues for structural modifications that can improve the activity. Docking study of the compounds 12, 14, and 16 into the active site of the topoisomerase II DNA gyrase enzymes revealed a similar binding mode to bound inhibitor Clorobiocin.
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