ABSTRACT
Objective: To search for the small molecule inhibitor with anti-tumor activity by fibroblast growth factor receptor 1 (FGFR1) as target. Methods: The analogue B6 of EF24 was obtained by reforming mono carbonyl curcumin analogues and applied to identifying the target with FGFR1 kinase activity assay. The effect of EF24 and its analogue B6 on the proliferation of HL7702 in normal human and four tumor cells, such as NCI-H460, SGC-7901, A549, and U251; With the concentration of 2.5, 5, and 10 μmol/L, B6 was used to investigate the phosphorylation inhibition of bFGF/FGFR downstream signal protein expression in NCI-H460 cells and Caspase-3 factor expression. Results: With the FGFR1 as target, B6 could inhibit the phosphorylation of FGFR1 in NCI-H460 cells, AKT, and ERK1/2; It also could inhibit the proliferation of cancer cells and promote cell apoptosis. Conclusion: The analogue B6 of EF24 is obtained from the leading compound EF24 with in vitro anti-tumor effect, which provides the basis of looking for the candidate anti-tumor drugs of FGFR1 inhibitor.