| Summary: | The aim of this study was to determine the cytotoxic effect of 3-arylidenechromanone (<b>1</b>) and 3-arylideneflavanone (<b>2</b>) on HL-60 and NALM-6 cell lines (two human leukemia cell lines) and a WM-115 melanoma cell line. Both compounds exhibited high cytotoxic activity with higher cytotoxicity exerted by compound <b>2</b>, for which IC<sub>50</sub> values below 10 µM were found for each cell line. For compound <b>1</b>, the IC<sub>50</sub> values were higher than 10 µM for HL-60 and WM-115 cell lines, but IC<sub>50</sub> < 10 µM was found for the NALM-6 cell line. Both compounds, at the concentrations close to IC<sub>50</sub> (concentration range: 5⁻24 µM/L for compound <b>1</b> and 6⁻10 µM/L for compound <b>2</b>), are not toxic towards red blood cells. The synthesized compounds were characterized using spectroscopic methods <sup>1</sup>H- and <sup>13</sup>C-NMR, IR, MS, elemental analysis, and X-ray diffraction. The lipophilicity of both synthesized compounds was determined using an RP-TLC method and the log<i>P</i> values found were compared with the theoretical ones taken from the Molinspiration Cheminformatics (miLog<i>P</i>) software package. The mode of binding of both compounds to human serum albumin was assessed using molecular docking methods.
|
|---|