In vitro: |
J. Enzym. Inhib. Med.Chem., 2015(3):1-6. | Synthesis and biological evaluation of 1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one and its aminomethyl derivatives.[Pubmed: 25068729 ] | Aminomethyl derivatives of 1,5-Bis(4-hydroxy-3-methoxyphenyl)penta-1,4-diene-3-one, designed as new cytotoxins, were synthesized and evaluated in terms of their cytotoxic activities. METHODS AND RESULTS: The compounds have low CC50 values in the low micromolar range against HL-60 neoplasms and HSC-2, HSC-3 and HSC-4 carcinoma cells. In general, the average CC50 values of these compounds were higher towards HGF, HPC and HPLF non-malignant cells, which reveals the tumour-selectivity of these aminomethyl derivatives, Mannich bases.
CONCLUSIONS:
Using specific concentrations of compounds 4 and 6 caused cleavage of PARP1 in HSC-2 cells but not HGF cells, which may be a contributing factor to cytotoxicities and the tumour-selectivities. |
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