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Bioorg Med Chem. 2016 Mar 15;24(6):1292-7. doi: 10.1016/j.bmc.2016.01.056. Epub 2016 Feb 1.

4H-Chromene-based anticancer agents towards multi-drug resistant HL60/MX2 human leukemia: SAR at the 4th and 6th positions.

Author information

1
Department of Medicinal Chemistry, University of Minnesota, 2231 6th Street SE, Minneapolis, MN 55455, USA.
2
Department of Medicinal Chemistry, University of Minnesota, 2231 6th Street SE, Minneapolis, MN 55455, USA; College of Traditional Chinese Veterinary Medicine, Agricultural University of Hebei, Baoding, Hebei 071001, People's Republic of China.
3
Department of Medicinal Chemistry, University of Minnesota, 2231 6th Street SE, Minneapolis, MN 55455, USA; LG Life Sciences Ltd, 104-1, Munji-dong, Yuseong-gu, Daejeon 305-380, South Korea.
4
Department of Medicinal Chemistry, University of Minnesota, 2231 6th Street SE, Minneapolis, MN 55455, USA. Electronic address: xingx009@umn.edu.

Abstract

4H-Chromene-based compounds, for example, CXL017, CXL035, and CXL055, have a unique anticancer potential that they selectively kill multi-drug resistant cancer cells. Reported herein is the extended structure-activity relationship (SAR) study, focusing on the ester functional group at the 4th position and the conformation at the 6th position. Sharp SARs were observed at both positions with respect to cellular cytotoxic potency and selectivity between the parental HL60 and the multi-drug resistant HL60/MX2 cells. These results provide critical guidance for future medicinal optimization.

KEYWORDS:

4H-Chromene; Anticancer; Cytotoxicity; Multi-drug resistant; Structure–activity relationship

PMID:
26867486
PMCID:
PMC6131690
DOI:
10.1016/j.bmc.2016.01.056
[Indexed for MEDLINE]
Free PMC Article

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