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Title: Tumour-specific cytotoxicity and structure-activity relationships of novel 1-[3-(2-methoxyethylthio)propionyl]-3,5-bis(benzylidene)-4-piperidones
Authors: Hossain, Mohammad ×
Das, Umashankar
Umemura, Naoki
Sakagami, Hiroshi
Balzarini, Jan
De Clercq, Erik
Kawase, Masami
Dimmock, Jonathan R #
Issue Date: May-2016
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:24 issue:10 pages:2206-14
Article number: 10.1016/j.bmc.2016.03.056
Abstract: A series of 1-acyl-3,5-bis(benzylidene)-4-piperidones 3-7 were designed and synthesized as novel cytotoxic agents. These compounds displayed potent cytotoxic properties towards human Molt4/C8, CEM, HSC-2, HSC-3 and HSC-4 neoplasms and also to murine L1210 cells. The majority of the compounds have sub-micromolar or very low micromolar IC50 and CC50 values and are significantly more potent than the reference alkylating drug melphalan. Evaluation of these compounds against non-malignant HGF and HPLF cells revealed the tumour-specific toxicity. In particular, 3e emerged as a promising lead cytotoxic agent which caused apoptosis and PARP1 cleavage in HSC-2 cells.
URI: 
ISSN: 0968-0896
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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