1-(3-Aminomethyl-4-hydroxyphenyl)-3-pyridinyl-2-propen-1-ones: A novel group of tumour-selective cytotoxins
Özet
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 CC 50 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.
Anahtar kelimeler
Atıf için künye
Bilginer, S., Gül, H. İ., Mete, E., Das, U., Sakagamı, H., Umemura, N., & Dimmock, J. R. (2013). 1-(3-Aminomethyl-4-hydroxyphenyl)-3-pyridinyl-2-propen-1-ones: A novel group of tumour-selective cytotoxins. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 28(5), 974–980. https://doi.org/10.3109/14756366.2012.700927
BibTeX
@article{bilginer2013-19917,
author = {Bilginer, Sinan and Gül, Halise İnci and Mete, Ebru and Das, Umashankar and Sakagamı, Hiroshi and Umemura, Naoki and Dimmock, Jonathan Richard},
title = {1-(3-Aminomethyl-4-hydroxyphenyl)-3-pyridinyl-2-propen-1-ones: A novel group of tumour-selective cytotoxins},
journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
year = {2013},
volume = {28},
number = {5},
pages = {974--980},
issn = {1475-6366},
doi = {10.3109/14756366.2012.700927},
url = {https://akademik.atauni.edu.tr/yayinlar/19917-1-3-aminomethyl-4-hydroxyphenyl-3-pyridinyl-2-propen-1-ones-a-novel-group-of}
}