Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 4, Pages 1563-1572Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.01.001
Keywords
4-Piperazinylquinoline; Isatin; Mannich base; Breast cancer cells; Anti-breast cancer activity; Hybrid pharmacophore approach
Funding
- Natural Sciences and Engineering Council of Canada (NSERC)
- Northern Cancer Research Foundation
- Ontario Ministry of Research and Innovation
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A novel class of 4-piperazinylquinoline derivatives based on the isatin scaffold were designed by molecular hybridization approach and synthesized for biological evaluation. Subsequently, the compounds were examined for their cytotoxic effects on two human breast tumor cell lines, MDA-MB468 and MCF7, and two non-cancer breast epithelial cell lines, 184B5 and MCF10A. Although all compounds examined were quite effective on the breast cancer cell lines examined, the compound 4-bromo-1-[4(7-chloro-quinolin-4-yl)-piperazin-1-ylmethyl]-1H-indole-2,3-dione (5b) and N-1-[4-(7-trifluoromethylquinolin4-yl)]-piperazin-1-ylmethyl-4-chloro-1H-indole-2,3-dione-3-thiosemicarbazone (8a) emerged as the most active among this series. It appeared that both 5b and 8a caused apoptosis to MCF7 cancer cells, but not MCF10A non-cancer cells. Thus, 4-piperazinylquinoline linked isatin analog can serve as the prototype molecule for further development of a new class of anti-breast cancer agents. (C) 2010 Elsevier Ltd. All rights reserved.
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