1-(3-Aminomethyl-4-hydroxyphenyl)-3-pyridinyl-2-propen-1-ones: A novel group of tumour-selective cytotoxins. (1st October 2013)

• Record Type: Journal Article
• Authors: Bilginer, Sinan; Gul, Halise Inci; Mete, Ebru; Das, Umashankar; Sakagami, Hiroshi; Umemura, Naoki; Dimmock, Jonathan Richard
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 28:Number 5(2013:Oct.)
• Page Start: 974
• Page End: 980
• Publication Date: 2013-10-01
• Subjects: Mannich bases -- azachalcones -- cytotoxicity -- molecular modelling -- PARP1; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2012.700927
• Languages: English
• ISSNs: 1475-6366

Abstract

Abstract : Two series of 1-(3-aminomethyl-4-hydroxyphenyl)-3-pyridinyl-2-propen-1-ones, designed as novel cytotoxins, were synthesized. The compounds had low CC50 values in the micromolar range against HL-60 promyelocytic leukemic cells and HSC-2, HSC-3 and HSC-4 oral squamous cell carcinomas. The CC50 values of these compounds were higher towards non-malignant HGF (gingival fibroblasts), HPC (pulp cells), and HPLF (periodontal ligament fibroblasts) cells, which reveals the tumour-selectivity of these enones. A representative compound 4c caused cleavage of PARP1 in HSC-2 cells but not in HGF cells, which may be a contributing factor to the tumour-selectivity.