- Tumour-specific cytotoxicity and structure-activity relationships of novel 1-[3-(2-methoxyethylthio)propionyl]-3,5-bis(benzylidene)-4-piperidones.
Tumour-specific cytotoxicity and structure-activity relationships of novel 1-[3-(2-methoxyethylthio)propionyl]-3,5-bis(benzylidene)-4-piperidones.
Bioorganic & medicinal chemistry (2016-04-14)
Mohammad Hossain, Umashankar Das, Naoki Umemura, Hiroshi Sakagami, Jan Balzarini, Erik De Clercq, Masami Kawase, Jonathan R Dimmock
PMID27073056
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.
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Supelco
Discovery® C8 Supelguard Guard Cartridge Kit, 5 μm particle size, L × I.D. 2 cm × 4 mm, contains 2 nuts, 2 ferrules, 5cm tubing, 1 guard cartridge and 1 guard holder