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Discovery of a uracil-derived small organic ligand with cytotoxic effect on human pc-3 cell lines via apoptosis

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ÇEÇENER, GÜLŞAH
Balaban, Rümeysa
Çeçener, Gülşah

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Poslu, Ayse Haliç
Nalbantsoy, Ayşe
Ertik, Onur
Koz, Ömer
Koz, Gamze

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Wiley-v C H Verlag Gmbh

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Abstract

A series of novel 6-amino-5-salicylidene uracils (1-19) were efficiently synthesized from the condensation reaction of 5,6-diamino-1,3-dimethyluracil with substituted salicylaldehydes. The structural characterization of the compounds was performed with spectroscopic methods and elemental analysis. All compounds were evaluated for their in vitro cytotoxic activity against PC-3 (human prostate adenocarcinoma), A549 (human alveolar adenocarcinoma) and SHSY-5Y (human neuroblastoma) cancer cell lines. 3,5-di-tert-Butylsalicylaldehyde derived salicylideneuracil (6ASU-8) showed promising cytotoxic activity against PC-3 cells with an IC50 value of 1.53 +/- 1.01 mu M, compared to doxorubicin, which had an IC50 value of 3.77 +/- 1.34 mu M. 6ASU-8 induced cell cycle arrest at the G2/M phase and promoted apoptosis in PC-3 cells (p<0.05*). Molecular docking results supported the experimental data, indicating that 6ASU-8 is more effective than doxorubicin. Additionally, in silico ADME analysis revealed that 6ASU-8 possesses acceptable predictive physicochemical properties.

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Prostate-cancer cells, Doxorubicin, Inhibitors, Growth, 5-aminouracil, Pyrimidine, Complexes, Uracil, Cytotoxicity, Pc-3, Apoptosis, Molecular docking, Science & technology, Physical sciences, Chemistry, multidisciplinary, Chemistry

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