The application belongs to the technical field of pharmaceutical
chemistry, and specifically discloses a
chalcone derivative and a preparation method thereof. 2,4-dihydroxy
formaldehyde is used as an initial
raw material, isopentenyl is introduced into 2,4-dihydroxybenzaldehyde through a Friedel-Crafts reaction, and then a heterocycle is introduced through a hydroxy
aldehyde condensation reaction of the heterocycle-substituted
formaldehyde, so that a
chalcone structure is formed. The prepared
chalcone derivative has a
structural formula as shown in Formula I, and the physicochemical properties thereof are studied. It is proved that the chalcone derivatives I-4, I-5, I-7, I-8, I-9, I-10, I-11, I-12 and I-14 all show a strong
inhibitory effect on the proliferation of four
tumor cells (PC9, MDA-MB-231, SMMC-7721 and SGC-7901). Among them, the
chalcone derivative I-4 can effectively inhibit the proliferation of
human lung cancer PC9 and H1975 cells in a concentration-
dependent manner, and shows good in-vivo anti-tumor activity and can induce iron death of
human lung cancer PC9 and H1975 cells, and has a good application prospect as an
anticancer drug.