Design synthesis and photophysical properties of a novel antitumor fluorescence agents

Abstract

Abstract Four novel fluorescent antitumor compounds were synthesized in three steps. In this paper, boron fluoride was introduced into the side bond of pyrimidine ring through a simple synthetic route, which enhanced the fluorescence intensity and anti-tumor activity. Through MTT test, the IC50 values of the four compounds reached the expected effect. Compound L4, in particular, had an IC50 value of 19.24 ± 5.88 in HeLa cells, which was slightly higher than that of 5-fluorouracil. Flow cytometry analysis showed that the four compounds had the ability to induce apoptosis of tumor cells, and compound L4 induced early apoptosis of Hela cells accounted for 31.3%. At the same time, molecular docking were carried out of four compounds by Molecular operating environment (MOE) software package version AutoDock Vina 1.1.2. The results show that hydrogen bond, π-π bonding and T-π bonding are the main forces. This provides a new idea for tumor therapy and potential for rapid identification of drug concentration in cells.