Title: Niacin esters of chalcones with tumor-selective properties
Authors: Panda, Atulya K
Das, Umashankar ×
Roayapalley, Praveen K
Sakagami, Hiroshi
Kawase, Masami
Balzarini, Jan
De Clercq, Erik
Dimmock, Jonathan R #
Issue Date: Dec-2016
Publisher: Taylor & Francis
Series Title: Journal of Enzyme Inhibition and Medicinal Chemistry vol:31 issue:6 pages:1451-1456
Article number: 10.3109/14756366.2016.1144595
Abstract: Novel series of niacin esters of chalcones 2, 4 and 6 were designed as antineoplastic agents that have the potential to release the chemoprotectant niacin. These enones are cytotoxic to human CD4(+ )T-lymphocyte Molt 4/C8 and CEM and murine leukemia L1210 cells. Quantitative structure-activity relationship (QSAR) studies of the biodata in series 4 revealed that cytotoxic potency was enhanced by placing electron-repelling groups in one of the aryl rings. The compounds are lethal to HL-60, HSC-2, HSC-3 and HSC-4 neoplasms but less toxic to nonmalignant hepatocyte growth factor, hematopoietic progenitor cell and human periodontal ligament fibroblast cells. Hence, the compounds display tumor-selective toxicity. These chalcones are well tolerated in mice and no overt toxicity was noted. The results establish that in general the compounds in series 2, 4 and 6 have positive characteristics which warrant further studies.
ISSN: 1475-6366
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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